DGIdb - BTK Gene Record

BTK 695 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

695
BRUTON TYROSINE KINASE
BTK
AGMX1
AT
ATK
BPK
IMD1
PSCTK1
XLA
300300
1133
ENSG00000010671
OTTHUMG00000022022
Q06187
TYROSINE-PROTEIN KINASE BTK
BTK_HUMAN
B-cell progenitor kinase
Agammaglobulinemia tyrosine kinase
65
1948
TYROSINE-PROTEIN KINASE BTK (EC 2.7.1.112) (BRUTON'S TYROSINE KINASE) (AGAMMAGLOBULINAEMIA TYROSINE KINASE) (ATK) (B CELL PROGENITOR KINASE) (BPK). [SOURCE:UNIPROT/SWISSPROT;ACC:Q06187]
NP_000052
NM_000061
BE0001284
PA25454
T25005

Gene Info:

Interpro Short Name	Ser-Thr/Tyr_kinase_cat_dom
Uniprot Status	Swiss-Prot
Human Readable Name	KINASE
Interpro Type	Domain
Interpro Name	Serine-threonine/tyrosine-protein kinase catalytic domain
Uniprot Evidence	1: Evidence at protein level
Human Readable Name	DRUGGABLE GENOME
Interpro Acc	IPR001245
GuideToPharmacology Gene Category Name	Tec family
GuideToPharmacology Gene Category ID	629
Target Class	Enzymes
Target Subclass	EC:2.7.10.2
Initial Gene Query	BTK
Counted Citations from 1950-2000	808
Gene Biotype	PROTEIN_CODING

(22 More Sources)

Gene Categories: Category Details

KINASE
TYROSINE KINASE
DRUG RESISTANCE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE
ENZYME
TRANSCRIPTION FACTOR

Publications:

Tam CS et al., 2019, Phase 1 study of the selective BTK inhibitor zanubrutinib in B-cell malignancies and safety and efficacy evaluation in CLL., Blood
Tarantelli C et al., 2019, The Bruton tyrosine kinase inhibitor zanubrutinib (BGB-3111) demonstrated synergies with other anti-lymphoma targeted agents., Haematologica
Guo Y et al., 2019, Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase., J Med Chem
Maddocks et al., 2015, Etiology of Ibrutinib Therapy Discontinuation and Outcomes in Patients With Chronic Lymphocytic Leukemia., JAMA Oncol
Sharma et al., 2016, Identification of a structurally novel BTK mutation that drives ibrutinib resistance in CLL., Oncotarget
Woyach et al., 2014, Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib., N. Engl. J. Med.
Sivina M et al., 2014, The bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) blocks hairy cell leukaemia survival, proliferation and B cell receptor signalling: a new therapeutic approach., Br J Haematol
Kim et al., 2015, Ibrutinib: a review of its use in patients with mantle cell lymphoma or chronic lymphocytic leukaemia., Drugs
Burger et al., 2016, Clonal evolution in patients with chronic lymphocytic leukaemia developing resistance to BTK inhibition., Nat Commun
Puig de la Bellacasa R et al., 2014, 4-Amino-2-arylamino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]pyrimidin-7-(8H)-ones as BCR kinase inhibitors for B lymphoid malignancies., Eur J Med Chem
Bamborough et al., 2008, Assessment of chemical coverage of kinome space and its implications for kinase drug discovery., J. Med. Chem.
Hantschel O et al., 2007, The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib., Proc Natl Acad Sci U S A
Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

SPEBRUTINIB BESYLATE BTK

Interaction Score: 4.48

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase BTK inhibitor

Trial Name AVL-292

PMIDs:
None found

Sources:
TdgClinicalTrial TTD ChemblInteractions
TIRABRUTINIB BTK

Interaction Score: 4.48

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions

VECABRUTINIB BTK

Interaction Score: 2.99

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Biochemical assay measuring inhibition of phosphorylation of a fluorescein-labeled polyGAT peptide, in the presence of active BTK enzyme, ATP, and inhibitor.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology

BMS-986142 BTK

Interaction Score: 2.99

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology
FENEBRUTINIB BTK

Interaction Score: 2.99

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology
CHEMBL228043 BTK

Interaction Score: 1.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction IN a cell-free BTK assay using BTK immunoprecipitated from B18.2 cells.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
EVOBRUTINIB BTK

Interaction Score: 1.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Binned value derived from a time-dependent BTK enzyme assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
BRANEBRUTINIB BTK

Interaction Score: 1.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Evaluated in a FLIPR calcium mobilisation assay in Ramos B lymphocytes.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
HM-71224 BTK

Interaction Score: 1.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase BTK inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
MSC-2364447 BTK

Interaction Score: 1.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase BTK inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
IBRUTINIB BTK

Interaction Score: 1.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family BTK inhibitor

Alteration BTK:C481S

Alteration BTK:C481.

PMIDs:
26182309 27626698 24869598 24697238 25802231 27199251 25222877

Sources:
DTC PharmGKB DoCM TdgClinicalTrial CIViC TTD DrugBank COSMIC MyCancerGenome GuideToPharmacology ChemblInteractions CGI
POSELTINIB BTK

Interaction Score: 0.75

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Biochemical assay result. Binned IC<sub>50</sub> value provided in patent.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
SPEBRUTINIB BTK

Interaction Score: 0.75

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology
ZANUBRUTINIB BTK

Interaction Score: 0.6

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of the enzymatic activity of recombinant human BTK in a TR-FRET assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
31340982 30679329 31381333

Sources:
TTD DrugBank GuideToPharmacology
CHEMBL23552 BTK

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17139284 17016423

Sources:
DrugBank
ABIVERTINIB BTK

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
ACALABRUTINIB BTK

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
TTD DrugBank GuideToPharmacology
XL-418 BTK

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
CHEMBL202721 BTK

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
AZD-1152-HQPA BTK

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB BTK

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17684099

Sources:
DTC DrugBank
MLN-8054 BTK

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL406845 BTK

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CENISERTIB BTK

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
DTC TALC MyCancerGenome
HESPERADIN BTK

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
19035792

Sources:
DTC
R-406 BTK

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25222877

Sources:
DTC
CHEMBL1997335 BTK

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ALISERTIB BTK

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PD-0166285 BTK

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB BTK

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ENTRECTINIB BTK

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TOZASERTIB BTK

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RG-1530 BTK

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB BTK

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAE-684 BTK

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PF-00562271 BTK

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ILORASERTIB BTK

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
FOSTAMATINIB BTK

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
26516587

Sources:
DrugBank

Ensembl: ENSG00000010671
- Version: 101_38
Alternate Names:

BTK Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: Q06187
- Version: 11-September-2012
Alternate Names:

695 Entrez Gene Id

BTK_HUMAN Uniprot Id

Q06187 Uniprot Accession

Gene Info:

Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom

Uniprot Status Swiss-Prot

Human Readable Name KINASE

Gene Categories:

KINASE, DRUGGABLE GENOME

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

695 Entrez Gene ID

Gene Info:

Initial Gene Query BTK

Counted Citations from 1950-2000 808

Gene Categories:

KINASE

Publications:
TdgClinicalTrial: Q06187
- Version: January-2014
Alternate Names:

BTK Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:2.7.10.2

Publications:

RussLampel: ENSG00000010671

Version: 26-July-2011

Alternate Names:

ENSG00000010671 Ensembl Gene Id

TYROSINE-PROTEIN KINASE BTK (EC 2.7.1.112) (BRUTON'S TYROSINE KINASE) (AGAMMAGLOBULINAEMIA TYROSINE KINASE) (ATK) (B CELL PROGENITOR KINASE) (BPK). [SOURCE:UNIPROT/SWISSPROT;ACC:Q06187] Description

BTK Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

GuideToPharmacology: 695
- Version: 29-September-2020
Alternate Names:

1133 HUGO Gene ID

1133 HUGO Gene Symbol

Bruton tyrosine kinase HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Tec family

GuideToPharmacology Gene Category ID 629

Gene Categories:

ENZYME

Publications:

PharmGKB: BTK

Version: 18-August-2020

Alternate Names:

PA25454 PharmGKB ID

Gene Info:

Publications:

Woyach et al., 2014, Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib., N. Engl. J. Med.

Sivina M et al., 2014, The bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) blocks hairy cell leukaemia survival, proliferation and B cell receptor signalling: a new therapeutic approach., Br J Haematol

CIViC: BTK

Version: 14-September-2020

Alternate Names:

695 Entrez Gene ID

65 CIViC Gene ID

Gene Info:

Gene Categories:

DRUG RESISTANCE

Publications:

Maddocks et al., 2015, Etiology of Ibrutinib Therapy Discontinuation and Outcomes in Patients With Chronic Lymphocytic Leukemia., JAMA Oncol

Sharma et al., 2016, Identification of a structurally novel BTK mutation that drives ibrutinib resistance in CLL., Oncotarget

Woyach et al., 2014, Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib., N. Engl. J. Med.

DrugBank: BE0001284

Version: 5.1.7

Alternate Names:

BTK DrugBank Gene Name

Q06187 UniProt Accession

695 Entrez Gene Id

Gene Info:

Publications:

Hantschel O et al., 2007, The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib., Proc Natl Acad Sci U S A

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

TTD: Tyrosine-protein kinase BTK
- Version: 2020.06.01
Alternate Names:

ATK TTD Gene Abbreviation

T25005 TTD Target ID

Gene Info:

Publications:

Dubovsky JA et al., 2013, Ibrutinib is an irreversible molecular inhibitor of ITK driving a Th1-selective pressure in T lymphocytes., Blood

CGI: BTK

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Woyach et al., 2014, Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib., N. Engl. J. Med.

Burger et al., 2016, Clonal evolution in patients with chronic lymphocytic leukaemia developing resistance to BTK inhibition., Nat Commun

DoCM: BTK
- Version: 27-September-2017
Alternate Names:

Gene Info:

Publications:

Woyach et al., 2014, Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib., N. Engl. J. Med.

DTC: BTK

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Bamborough et al., 2008, Assessment of chemical coverage of kinome space and its implications for kinase drug discovery., J. Med. Chem.

Puig de la Bellacasa R et al., 2014, 4-Amino-2-arylamino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]pyrimidin-7-(8H)-ones as BCR kinase inhibitors for B lymphoid malignancies., Eur J Med Chem

Hantschel O et al., 2007, The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib., Proc Natl Acad Sci U S A

HingoraniCasas: ENSG00000010671
- Version: 31-May-2017
Alternate Names:

ENSG00000010671 Gene Symbol

BTK Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

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

BTK Gene Symbol

Gene Info:

Publications:
ChemblInteractions: AGMX1
- Version: chembl_23
Alternate Names:

ATK GENE_SYMBOL

BPK GENE_SYMBOL

BTK GENE_SYMBOL

Gene Info:

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

695 Entrez Gene Id

BTK MyCancerGenome Gene Symbol

BTK MyCancerGenome Reported Gene Name

Gene Info:

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

Tyrosine-protein kinase BTK Gene Name

Q06187 UniProt ID

Gene Info:

Gene Categories:

KINASE, TRANSCRIPTION FACTOR

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

AGMX1 GO Gene Synonym

ATK GO Gene Synonym

BPK GO Gene Synonym

Gene Info:

Gene Categories:

TYROSINE KINASE

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

BTK Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

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

695 Gene ID

AGMX1 dGene Synonym

AT dGene Synonym

Gene Info:

Gene Categories:

KINASE, TYROSINE KINASE

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

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

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

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

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

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

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

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
COSMIC: BTK
- Version: 4-Sep-2020
Alternate Names:

Gene Info:

Gene Categories:

DRUG RESISTANCE

Publications:

Direct Interaction	yes
Mechanism of Interaction	Tyrosine-protein kinase BTK inhibitor
Trial Name	AVL-292

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

Details of the Assay for Interaction	Biochemical assay measuring inhibition of phosphorylation of a fluorescein-labeled polyGAT peptide, in the presence of active BTK enzyme, ATP, and inhibitor.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	IN a cell-free BTK assay using BTK immunoprecipitated from B18.2 cells.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	Binned value derived from a time-dependent BTK enzyme assay.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	Evaluated in a FLIPR calcium mobilisation assay in Ramos B lymphocytes.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Drug family	BTK inhibitor
Alteration	BTK:C481S
Alteration	BTK:C481.

Details of the Assay for Interaction	Biochemical assay result. Binned IC<sub>50</sub> value provided in patent.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	Inhibition of the enzymatic activity of recombinant human BTK in a TR-FRET assay.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	In a biochemical assay.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

ENSG00000010671	Ensembl Gene Id
TYROSINE-PROTEIN KINASE BTK (EC 2.7.1.112) (BRUTON'S TYROSINE KINASE) (AGAMMAGLOBULINAEMIA TYROSINE KINASE) (ATK) (B CELL PROGENITOR KINASE) (BPK). [SOURCE:UNIPROT/SWISSPROT;ACC:Q06187]	Description
BTK	Display Id

1133	HUGO Gene ID
1133	HUGO Gene Symbol
Bruton tyrosine kinase	HUGO Gene Name

BTK	DrugBank Gene Name
Q06187	UniProt Accession
695	Entrez Gene Id

695	Entrez Gene Id
BTK	MyCancerGenome Gene Symbol
BTK	MyCancerGenome Reported Gene Name

BTK Gene Record

BTK 695 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Tyrosine-protein kinase BTK inhibitor Trial Name AVL-292

PMIDs: None found

Sources: TdgClinicalTrial TTD ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Biochemical assay measuring inhibition of phosphorylation of a fluorescein-labeled polyGAT peptide, in the presence of active BTK enzyme, ATP, and inhibitor. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: TTD GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: TTD GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: TTD GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction IN a cell-free BTK assay using BTK immunoprecipitated from B18.2 cells. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Binned value derived from a time-dependent BTK enzyme assay. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Evaluated in a FLIPR calcium mobilisation assay in Ramos B lymphocytes. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Tyrosine-protein kinase BTK inhibitor

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Tyrosine-protein kinase BTK inhibitor

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Drug family BTK inhibitor Alteration BTK:C481S Alteration BTK:C481.

PMIDs: 26182309 27626698 24869598 24697238 25802231 27199251 25222877

Sources: DTC PharmGKB DoCM TdgClinicalTrial CIViC TTD DrugBank COSMIC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Biochemical assay result. Binned IC<sub>50</sub> value provided in patent. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of the enzymatic activity of recombinant human BTK in a TR-FRET assay. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: 31340982 30679329 31381333

Sources: TTD DrugBank GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17139284 17016423

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction In a biochemical assay. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: TTD DrugBank GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase BTK inhibitor

Trial Name AVL-292

PMIDs:
None found

Sources:
TdgClinicalTrial TTD ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Biochemical assay measuring inhibition of phosphorylation of a fluorescein-labeled polyGAT peptide, in the presence of active BTK enzyme, ATP, and inhibitor.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction IN a cell-free BTK assay using BTK immunoprecipitated from B18.2 cells.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Binned value derived from a time-dependent BTK enzyme assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Evaluated in a FLIPR calcium mobilisation assay in Ramos B lymphocytes.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase BTK inhibitor

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase BTK inhibitor

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family BTK inhibitor

Alteration BTK:C481S

Alteration BTK:C481.

PMIDs:
26182309 27626698 24869598 24697238 25802231 27199251 25222877

Sources:
DTC PharmGKB DoCM TdgClinicalTrial CIViC TTD DrugBank COSMIC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Biochemical assay result. Binned IC<sub>50</sub> value provided in patent.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of the enzymatic activity of recombinant human BTK in a TR-FRET assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
31340982 30679329 31381333

Sources:
TTD DrugBank GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
17139284 17016423

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
TTD DrugBank GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
17684099

Sources:
DTC DrugBank

Interaction Types & Directionality:

n/a