DGIdb - CDK4 Gene Record

CDK4 1019 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

1019
CYCLIN DEPENDENT KINASE 4
CDK4
CMM3
PSK-J3
123829
1773
ENSG00000135446
OTTHUMG00000170382
CDK 4,6
CDK 1,2,4,5,6,7,9 (pan-CDK)
P11802
cyclin-dependent kinase 4
CDK4_HUMAN
CELL DIVISION PROTEIN KINASE 4
1976
NP_000066
NM_000075
CELL DIVISION PROTEIN KINASE 4 (EC 2.7.1.37) (CYCLIN-DEPENDENT KINASE 4) (PSK-J3). [SOURCE:UNIPROT/SWISSPROT;ACC:P11802]
13
BE0002216
PA102
T85799

Gene Info:

Interpro Type	Domain
Uniprot Status	Swiss-Prot
Interpro Name	Serine/threonine- / dual-specificity protein kinase, catalytic domain
Human Readable Name	DRUGGABLE GENOME
Interpro Acc	IPR002290
Human Readable Name	KINASE
Interpro Short Name	Ser/Thr_dual-sp_kinase_dom
Uniprot Evidence	1: Evidence at protein level
GuideToPharmacology Gene Category Name	CDK4 subfamily
GuideToPharmacology Gene Category ID	488
Target Class	Enzymes
Target Subclass	EC:2.7.11.22
CancerCommons Reported Gene Name	CDK4/6
CancerCommons Reported Gene Name	Pan CDK
Initial Gene Query	CDK4
Counted Citations from 1950-2000	3030
Gene Biotype	PROTEIN_CODING

(26 More Sources)

Gene Categories: Category Details

TRANSCRIPTION FACTOR COMPLEX
TUMOR SUPPRESSOR
KINASE
SERINE THREONINE KINASE
DRUG RESISTANCE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE
ENZYME
TRANSCRIPTION FACTOR

Publications:

Rocca A et al., 2017, Progress with palbociclib in breast cancer: latest evidence and clinical considerations., Ther Adv Med Oncol
Olanich ME et al., 2015, CDK4 Amplification Reduces Sensitivity to CDK4/6 Inhibition in Fusion-Positive Rhabdomyosarcoma., Clin Cancer Res
Dickson et al., 2013, Phase II trial of the CDK4 inhibitor PD0332991 in patients with advanced CDK4-amplified well-differentiated or dedifferentiated liposarcoma., J. Clin. Oncol.
Dickson et al., 2016, Progression-Free Survival Among Patients With Well-Differentiated or Dedifferentiated Liposarcoma Treated With CDK4 Inhibitor Palbociclib: A Phase 2 Clinical Trial., JAMA Oncol
Perez et al., 2015, Efficacy of CDK4 inhibition against sarcomas depends on their levels of CDK4 and p16ink4 mRNA., Oncotarget
Logan et al., 2013, PD-0332991, a potent and selective inhibitor of cyclin-dependent kinase 4/6, demonstrates inhibition of proliferation in renal cell carcinoma at nanomolar concentrations and molecular markers predict for sensitivity., Anticancer Res.
Reddy MV et al., 2014, Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5)., J Med Chem
Fry et al., 2004, Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts., Mol. Cancer Ther.
Burgess A et al., 2006, Inhibition of S/G2 phase CDK4 reduces mitotic fidelity., J Biol Chem
Gelbert et al., 2014, Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine., Invest New Drugs
Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Rhee et al., 1995, c-Myc and cyclin D3 (CcnD3) genes are independent targets for glucocorticoid inhibition of lymphoid cell proliferation., Cancer Res.
Bortolozzi R et al., 2018, Ribociclib, a Cdk4/Cdk6 kinase inhibitor, enhances glucocorticoid sensitivity in B-acute lymphoblastic leukemia (B-All)., Biochem Pharmacol
Swarbrick et al., 2000, Cooperation of p27(Kip1) and p18(INK4c) in progestin-mediated cell cycle arrest in T-47D breast cancer cells., Mol. Cell. Biol.
Rader et al., 2013, Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma., Clin. Cancer Res.
Banerji et al., 2005, Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models., Clin. Cancer Res.
Park et al., 2000, Involvement of retinoblastoma family members and E2F/DP complexes in the death of neurons evoked by DNA damage., J. Neurosci.
Montagnoli A et al., 2008, A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity., Nat Chem Biol
Frazer-Abel et al., 2004, Nicotine activates nuclear factor of activated T cells c2 (NFATc2) and prevents cell cycle entry in T cells., J. Pharmacol. Exp. Ther.
Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect

CHEMBL1956069 CDK4

Interaction Score: 3.44

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16476733

Sources:
DTC
CHEMBL1956070 CDK4

Interaction Score: 2.58

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
16476733

Sources:
DTC GuideToPharmacology
LEROCICLIB CDK4

Interaction Score: 1.72

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of CDK4/cyclin D1

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology
G1T28-1 CDK4

Interaction Score: 1.72

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
TTD ChemblInteractions
FASCAPLYSIN CDK4

Interaction Score: 1.72

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology
RIVICICLIB CDK4

Interaction Score: 1.72

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Details of the Assay for Interaction CDK4/cyclin D1 complex

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions
RIBOCICLIB CDK4

Interaction Score: 1.29

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name LEE011

Novel drug target Novel Target

Specific Action of the Ligand Inhibition

PMIDs:
24045179 25810375 29408328

Sources:
ClearityFoundationBiomarkers TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions CGI
AG-24322 CDK4

Interaction Score: 1.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
TTD ChemblInteractions

ABEMACICLIB CDK4

Interaction Score: 0.98

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
24919854

Sources:
ClearityFoundationBiomarkers CancerCommons OncoKB TTD DrugBank GuideToPharmacology ChemblInteractions

RIBOCICLIB SUCCINATE CDK4

Interaction Score: 0.86

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PALBOCICLIB CDK4

Interaction Score: 0.62

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

Mechanism of Interaction CDK4/cyclin D1 inhibitor

Direct Interaction yes

PMIDs:
28203301 25810375 23569312 27124835 26528855 23898052 24417566 15542782

Sources:
CancerCommons MyCancerGenomeClinicalTrial DTC OncoKB CIViC DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions
PURVALANOL B CDK4

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11752352

Sources:
DrugBank
RG-547 CDK4

Interaction Score: 0.57

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TRILACICLIB CDK4

Interaction Score: 0.57

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of CDK4/cyclin D3

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology
ALVOCIDIB CDK4

Interaction Score: 0.55

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Novel drug target Novel Target

PMIDs:
11752352

Sources:
DTC TdgClinicalTrial DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions
MILCICLIB CDK4

Interaction Score: 0.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Details of the Assay for Interaction CDK4/cyclin D1 complex

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions
RGB-286638 CDK4

Interaction Score: 0.4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Details of the Assay for Interaction in association with cyclin D1

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions
VORUCICLIB CDK4

Interaction Score: 0.34

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of CDK4/cyclinD1.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions
APREMILAST CDK4

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
TANESPIMYCIN CDK4

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16203796

Sources:
NCI
PHA-793887 CDK4

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
TTD ChemblInteractions
AT-7519 CDK4

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclin-dependent kinase inhibitor

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions
BMS-387032 CDK4

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology
ALPELISIB CDK4

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25002028

Sources:
CIViC
CAMPTOTHECIN CDK4

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10777774

Sources:
NCI
UCN-01 CDK4

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
RONICICLIB CDK4

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AZD-5438 CDK4

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclin-dependent kinase inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
DEXAMETHASONE CDK4

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7664296 29408328

Sources:
NCI CIViC
NICOTINE CDK4

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15231866

Sources:
NCI
CHEMBL225519 CDK4

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18469809

Sources:
DTC
PROGESTERONE CDK4

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10713180

Sources:
NCI
FOSTAMATINIB CDK4

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
26516587

Sources:
DrugBank

Ensembl: ENSG00000135446
- Version: 101_38
Alternate Names:

CDK4 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P11802
- Version: 11-September-2012
Alternate Names:

CDK4 Uniprot Gene Name

1019 Entrez Gene Id

ENSG00000135446 Ensembl Gene Id

Gene Info:

Interpro Type Domain

Uniprot Status Swiss-Prot

Interpro Name Serine/threonine- / dual-specificity protein kinase, catalytic domain

Gene Categories:

KINASE, DRUGGABLE GENOME

Publications:
RussLampel: ENSG00000135446
- Version: 26-July-2011
Alternate Names:

CELL DIVISION PROTEIN KINASE 4 (EC 2.7.1.37) (CYCLIN-DEPENDENT KINASE 4) (PSK-J3). [SOURCE:UNIPROT/SWISSPROT;ACC:P11802] Description

ENSG00000135446 Ensembl Gene Id

CDK4 Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
CancerCommons: CDK4
- Version: 25-July-2013
Alternate Names:

1019 Entrez Gene ID

Gene Info:

CancerCommons Reported Gene Name CDK4/6

CancerCommons Reported Gene Name Pan CDK

Publications:
BaderLabGenes: CDK4
- Version: February-2014
Alternate Names:

1019 Entrez Gene ID

Gene Info:

Initial Gene Query CDK4

Counted Citations from 1950-2000 3030

Gene Categories:

KINASE

Publications:
TdgClinicalTrial: P11802
- Version: January-2014
Alternate Names:

CDK4 Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:2.7.11.22

Publications:
GuideToPharmacology: 1019
- Version: 29-September-2020
Alternate Names:

1773 HUGO Gene ID

1773 HUGO Gene Symbol

cyclin dependent kinase 4 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name CDK4 subfamily

GuideToPharmacology Gene Category ID 488

Gene Categories:

ENZYME

Publications:
PharmGKB: CDK4
- Version: 18-August-2020
Alternate Names:

PA102 PharmGKB ID

Gene Info:

Publications:

Stevens A et al., 2014, Pharmacogenomics of insulin-like growth factor-I generation during GH treatment in children with GH deficiency or Turner syndrome., Pharmacogenomics J

CIViC: CDK4

Version: 14-September-2020

Alternate Names:

1019 Entrez Gene ID

13 CIViC Gene ID

Gene Info:

Gene Categories:

DRUG RESISTANCE

Publications:

Olanich ME et al., 2015, CDK4 Amplification Reduces Sensitivity to CDK4/6 Inhibition in Fusion-Positive Rhabdomyosarcoma., Clin Cancer Res

Dickson et al., 2013, Phase II trial of the CDK4 inhibitor PD0332991 in patients with advanced CDK4-amplified well-differentiated or dedifferentiated liposarcoma., J. Clin. Oncol.

Dickson et al., 2016, Progression-Free Survival Among Patients With Well-Differentiated or Dedifferentiated Liposarcoma Treated With CDK4 Inhibitor Palbociclib: A Phase 2 Clinical Trial., JAMA Oncol

DrugBank: BE0002216

Version: 5.1.7

Alternate Names:

CDK4 DrugBank Gene Name

P11802 UniProt Accession

1019 Entrez Gene Id

Gene Info:

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Rocca A et al., 2017, Progress with palbociclib in breast cancer: latest evidence and clinical considerations., Ther Adv Med Oncol

Fry et al., 2004, Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts., Mol. Cancer Ther.

NCI: CDK4

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Grillo et al., 2006, Validation of cyclin D1/CDK4 as an anticancer drug target in MCF-7 breast cancer cells: Effect of regulated overexpression of cyclin D1 and siRNA-mediated inhibition of endogenous cyclin D1 and CDK4 expression., Breast Cancer Res. Treat.

Hu et al., 2001, Differential effects of transforming growth factor on cell cycle regulatory molecules in human myeloid leukemia cells., Oncogene

Banerji et al., 2005, Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models., Clin. Cancer Res.

DTC: CDK4

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Burgess A et al., 2006, Inhibition of S/G2 phase CDK4 reduces mitotic fidelity., J Biol Chem

Montagnoli A et al., 2008, A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity., Nat Chem Biol

Reddy MV et al., 2014, Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5)., J Med Chem

HingoraniCasas: ENSG00000135446
- Version: 31-May-2017
Alternate Names:

ENSG00000135446 Gene Symbol

CDK4 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
MyCancerGenome: CDK4
- Version: 20-Jun-2017
Alternate Names:

1019 Entrez Gene Id

CDK4 MyCancerGenome Gene Symbol

CDK 1,2,4,5,6,7,9 (pan-CDK) MyCancerGenome Reported Gene Name

Gene Info:

Publications:
TALC: CDK4
- Version: 12-May-2016
Alternate Names:

CDK4 Gene Symbol

Gene Info:

Publications:
ChemblInteractions: CDK4
- Version: chembl_23
Alternate Names:

CDK4 GENE_SYMBOL

Cyclin-dependent kinase 4 UNIPROT

Cell division protein kinase 4 UNIPROT

Gene Info:

Publications:
OncoKB: CDK4
- Version: 23-July-2020
Alternate Names:

1019 OncoKB Entrez Id

PSK-J3 OncoKB Gene Synonym

CMM3 OncoKB Gene Synonym

Gene Info:

Publications:
Pharos: CDK4
- Version: 03-September-2020
Alternate Names:

Cyclin-dependent kinase 4 Gene Name

P11802 UniProt ID

Gene Info:

Gene Categories:

KINASE, TRANSCRIPTION FACTOR

Publications:
Tempus: CDK4
- Version: 11-November-2018
Alternate Names:

CDK4 Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
dGene: CDK4
- Version: 27-Jun-2013
Alternate Names:

1019 Gene ID

CMM3 dGene Synonym

PSK-J3 dGene Synonym

Gene Info:

Gene Categories:

KINASE, SERINE THREONINE KINASE

Publications:
TTD: Cyclin-dependent kinase 4
- Version: 2020.06.01
Alternate Names:

CDK4 TTD Gene Abbreviation

T85799 TTD Target ID

Gene Info:

Publications:
CGI: CDK4
- Version: 27-September-2017
Alternate Names:

Gene Info:

Publications:
ClearityFoundationClinicalTrial: CDK4
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
MyCancerGenomeClinicalTrial: CDK4
- Version: 30-February-2014
Alternate Names:

Gene Info:

Publications:
ClearityFoundationBiomarkers: CDK4
- Version: 26-July-2013
Alternate Names:

Gene Info:

Publications:
MskImpact: CDK4
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FoundationOneGenes: CDK4
- Version: 03-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CarisMolecularIntelligence: CDK4
- Version: 04-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
GO: CDK4
- Version: 05-September-2020
Alternate Names:

Gene Info:

Gene Categories:

TRANSCRIPTION FACTOR COMPLEX, TUMOR SUPPRESSOR, DRUG RESISTANCE

Publications:
Oncomine: CDK4
- Version: v3
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	True

Details of the Assay for Interaction	Inhibition of CDK4/cyclin D1
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Mechanism of Interaction	Cyclin-dependent kinase 4 inhibitor
Direct Interaction	yes

Trial Name	LEE011
Novel drug target	Novel Target
Specific Action of the Ligand	Inhibition

Details of the Assay for Interaction	CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Reported Cancer Type	Melanoma
Mechanism of Interaction	CDK4/cyclin D1 inhibitor
Direct Interaction	yes

Details of the Assay for Interaction	Inhibition of CDK4/cyclin D3
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	Inhibition of CDK4/cyclinD1.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Mechanism of Interaction	Cyclin-dependent kinase inhibitor
Direct Interaction	yes

CDK4	Uniprot Gene Name
1019	Entrez Gene Id
ENSG00000135446	Ensembl Gene Id

CELL DIVISION PROTEIN KINASE 4 (EC 2.7.1.37) (CYCLIN-DEPENDENT KINASE 4) (PSK-J3). [SOURCE:UNIPROT/SWISSPROT;ACC:P11802]	Description
ENSG00000135446	Ensembl Gene Id
CDK4	Display Id

1773	HUGO Gene ID
1773	HUGO Gene Symbol
cyclin dependent kinase 4	HUGO Gene Name

CDK4	DrugBank Gene Name
P11802	UniProt Accession
1019	Entrez Gene Id

CDK4	GENE_SYMBOL
Cyclin-dependent kinase 4	UNIPROT
Cell division protein kinase 4	UNIPROT

1019	OncoKB Entrez Id
PSK-J3	OncoKB Gene Synonym
CMM3	OncoKB Gene Synonym

CDK4 Gene Record

CDK4 1019 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16476733

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

PMIDs: 16476733

Sources: DTC GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of CDK4/cyclin D1 Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: TTD GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes

PMIDs: None found

Sources: TTD ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes Details of the Assay for Interaction CDK4/cyclin D1 complex

PMIDs: None found

Sources: TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Trial Name LEE011 Novel drug target Novel Target Specific Action of the Ligand Inhibition

PMIDs: 24045179 25810375 29408328

Sources: ClearityFoundationBiomarkers TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions CGI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes

PMIDs: None found

Sources: TTD ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: 24919854

Sources: ClearityFoundationBiomarkers CancerCommons OncoKB TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Reported Cancer Type Melanoma Mechanism of Interaction CDK4/cyclin D1 inhibitor Direct Interaction yes

PMIDs: 28203301 25810375 23569312 27124835 26528855 23898052 24417566 15542782

Sources: CancerCommons MyCancerGenomeClinicalTrial DTC OncoKB CIViC DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11752352

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of CDK4/cyclin D3 Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: TTD GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes Novel drug target Novel Target

PMIDs: 11752352

Sources: DTC TdgClinicalTrial DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Direct Interaction yes Details of the Assay for Interaction CDK4/cyclin D1 complex

PMIDs: None found

Sources: GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor Details of the Assay for Interaction in association with cyclin D1

PMIDs: None found

Sources: TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of CDK4/cyclinD1. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

n/a

PMIDs:
16476733

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
16476733

Sources:
DTC GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of CDK4/cyclin D1

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
TTD ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Details of the Assay for Interaction CDK4/cyclin D1 complex

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name LEE011

Novel drug target Novel Target

Specific Action of the Ligand Inhibition

PMIDs:
24045179 25810375 29408328

Sources:
ClearityFoundationBiomarkers TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
TTD ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
24919854

Sources:
ClearityFoundationBiomarkers CancerCommons OncoKB TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

Mechanism of Interaction CDK4/cyclin D1 inhibitor

Direct Interaction yes

PMIDs:
28203301 25810375 23569312 27124835 26528855 23898052 24417566 15542782

Sources:
CancerCommons MyCancerGenomeClinicalTrial DTC OncoKB CIViC DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
11752352

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of CDK4/cyclin D3

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Novel drug target Novel Target

PMIDs:
11752352

Sources:
DTC TdgClinicalTrial DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Direct Interaction yes

Details of the Assay for Interaction CDK4/cyclin D1 complex

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclin-dependent kinase 4 inhibitor

Details of the Assay for Interaction in association with cyclin D1

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of CDK4/cyclinD1.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
16203796

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
TTD ChemblInteractions