DGIdb - CCKBR Gene Record

CCKBR 887 Druggable Genome

Alternate Names:

887
CHOLECYSTOKININ B RECEPTOR
CCKBR
CCK-B
CCK2R
GASR
118445
1571
ENSG00000110148
OTTHUMG00000133380
CCKRB
Gastrin/cholecystokinin type B receptor
Cholecystokinin-2 receptor
CCK-B receptor
CCK-BR
CCK2-R
P32239
GASR_HUMAN
GASTRIN/CHOLECYSTOKININ TYPE B RECEPTOR (CCK-B RECEPTOR) (CCK-BR) (CHOLECYSTOKININ-2 RECEPTOR) (CCK2-R). [SOURCE:UNIPROT/SWISSPROT;ACC:P32239]
BE0001158
77
CCK<sub>2</sub> receptor
NM_176875
NP_795344
PA26143
T05849

Gene Info:

Interpro Acc	IPR000276
Human Readable Name	G PROTEIN COUPLED RECEPTOR
Uniprot Status	Swiss-Prot
Interpro Type	Family
Interpro Short Name	7TM_GPCR_Rhodpsn
Uniprot Evidence	1: Evidence at protein level
Human Readable Name	DRUGGABLE GENOME
Interpro Name	GPCR, rhodopsin-like, 7TM
Target Class	Receptors
Target Subclass	GPCR
Target Subclass	Rhodopsin
GuideToPharmacology Gene Category Name	Cholecystokinin receptors
GuideToPharmacology Gene Category ID	15
Target Main Class	Receptors
Transmembrane Helix Count	7
Gene Biotype	PROTEIN_CODING

(10 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Tiwari AK et al., 2010, Association study of polymorphisms in cholecystokinin gene and its receptors with antipsychotic induced weight gain in schizophrenia patients., Prog Neuropsychopharmacol Biol Psychiatry
Håkanson et al., 1999, CCK2 receptor antagonists: pharmacological tools to study the gastrin-ECL cell-parietal cell axis., Regul. Pept.
Bock et al., 1994, Selective non-peptide ligands for an accommodating peptide receptor. Imidazobenzodiazepines as potent cholecystokinin type B receptor antagonists., Bioorg. Med. Chem.
Harikumar KG et al., 2010, Modulation of cell surface expression of nonactivated cholecystokinin receptors using bivalent ligand-induced internalization., J Med Chem
Scott et al., 2012, Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017)., J. Med. Chem.
Singh et al., 1986, Role of gastrin and gastrin receptors on the growth of a transplantable mouse colon carcinoma (MC-26) in BALB/c mice., Cancer Res.
Nishida et al., 1995, Gastrin receptor antagonist YM022 prevents hypersecretion after long-term acid suppression., Am. J. Physiol.
Makovec et al., 1992, Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives., J. Med. Chem.
Khan et al., 2004, Effect of repeat exposure on neuroendocrine and symptom responses to pentagastrin., Psychiatry Res
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Radu et al., 2002, Anxiogenic effects of the CCK(B) agonist pentagastrin in humans and dose-dependent increase in plasma C-peptide levels., Psychopharmacology (Berl.)
Xu et al., 1996, L-740,093, a new antagonist of the CCK-B receptor, potentiates the antinociceptive effect of morphine: electrophysiological and behavioural studies., Neuropeptides
Costall et al., 1991, Anxiolytic effects of CCK-B antagonists., Neuropeptides
Berna MJ et al., 2007, Role of CCK/gastrin receptors in gastrointestinal/metabolic diseases and results of human studies using gastrin/CCK receptor agonists/antagonists in these diseases., Curr Top Med Chem
Olszewska-Pazdrak et al., 2004, Epidermal growth factor potentiates cholecystokinin/gastrin receptor-mediated Ca2+ release by activation of mitogen-activated protein kinases., J. Biol. Chem.
Weng et al., 1996, Novel CCK-B receptor agonists: diketopiperazine analogues derived for CCK4 bioactive conformation., Regul. Pept.

PENTAGASTRIN CCKBR

Interaction Score: 27.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
3004700 7491961 1732532 15157745 11752352 12073167

Sources:
TEND TdgClinicalTrial TTD DrugBank
ITRIGLUMIDE CCKBR

Interaction Score: 8.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Cholecystokinin B receptor antagonist

Direct Interaction yes

PMIDs:
17584143

Sources:
TTD ChemblInteractions
L-365260 CCKBR

Interaction Score: 8.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
20235611

Sources:
DTC GuideToPharmacology
NETAZEPIDE CCKBR

Interaction Score: 8.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cholecystokinin B receptor antagonist

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions
CI-988 CCKBR

Interaction Score: 5.41

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cholecystokinin B receptor antagonist

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions
L-740093 CCKBR

Interaction Score: 2.71

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
LORGLUMIDE CCKBR

Interaction Score: 2.71

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CHEMBL117281 CCKBR

Interaction Score: 2.71

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
NASTORAZEPIDE CALCIUM CCKBR

Interaction Score: 2.71

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
AZD-4017 CCKBR

Interaction Score: 1.8

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22691057

Sources:
DTC
PD-170292 CCKBR

Interaction Score: 1.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CERULETIDE CCKBR

Interaction Score: 1.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
SPIROGLUMIDE CCKBR

Interaction Score: 1.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
DEVAZEPIDE CCKBR

Interaction Score: 1.35

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
BENZODIAZEPINE CCKBR

Interaction Score: 1.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10235629 7712133

Sources:
NCI
SINCALIDE CCKBR

Interaction Score: 0.9

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? True

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
DrugBank GuideToPharmacology
INOSITOL CCKBR

Interaction Score: 0.58

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14602717 8876029

Sources:
NCI
DIAZEPAM CCKBR

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1679211

Sources:
NCI
MORPHINE CCKBR

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8771563

Sources:
NCI
OLANZAPINE CCKBR

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20732371

Sources:
PharmGKB
CLOZAPINE CCKBR

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20732371

Sources:
PharmGKB

Ensembl: ENSG00000110148
- Version: 101_38
Alternate Names:

CCKBR Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:

RussLampel: ENSG00000110148

Version: 26-July-2011

Alternate Names:

GASTRIN/CHOLECYSTOKININ TYPE B RECEPTOR (CCK-B RECEPTOR) (CCK-BR) (CHOLECYSTOKININ-2 RECEPTOR) (CCK2-R). [SOURCE:UNIPROT/SWISSPROT;ACC:P32239] Description

CCKBR Display Id

ENSG00000110148 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

HopkinsGroom: P32239
- Version: 11-September-2012
Alternate Names:

GASTRIN/CHOLECYSTOKININ TYPE B RECEPTOR Uniprot Protein Name

P32239 Uniprot Accession

ENSG00000110148 Ensembl Gene Id

Gene Info:

Interpro Acc IPR000276

Human Readable Name G PROTEIN COUPLED RECEPTOR

Uniprot Status Swiss-Prot

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
TEND: P32239
- Version: 01-August-2011
Alternate Names:

CCKBR Gene Symbol

P32239 Uniprot Accession

ENSG00000110148 Ensembl Gene Id

Gene Info:

Target Main Class Receptors

Target Subclass Rhodopsin

Target Subclass GPCR

Publications:
TdgClinicalTrial: P32239
- Version: January-2014
Alternate Names:

CCKBR Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
GuideToPharmacology: 887
- Version: 29-September-2020
Alternate Names:

1571 HUGO Gene ID

1571 HUGO Gene Symbol

cholecystokinin B receptor HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Cholecystokinin receptors

GuideToPharmacology Gene Category ID 15

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

PharmGKB: CCKBR

Version: 18-August-2020

Alternate Names:

PA26143 PharmGKB ID

Gene Info:

Publications:

Tiwari AK et al., 2010, Association study of polymorphisms in cholecystokinin gene and its receptors with antipsychotic induced weight gain in schizophrenia patients., Prog Neuropsychopharmacol Biol Psychiatry

DrugBank: BE0001158

Version: 5.1.7

Alternate Names:

CCKBR DrugBank Gene Name

P32239 UniProt Accession

887 Entrez Gene Id

Gene Info:

Publications:

Singh et al., 1986, Role of gastrin and gastrin receptors on the growth of a transplantable mouse colon carcinoma (MC-26) in BALB/c mice., Cancer Res.

Nishida et al., 1995, Gastrin receptor antagonist YM022 prevents hypersecretion after long-term acid suppression., Am. J. Physiol.

Makovec et al., 1992, Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives., J. Med. Chem.

TTD: Gastrin/cholecystokinin type B receptor

Version: 2020.06.01

Alternate Names:

CCKBR TTD Gene Abbreviation

T05849 TTD Target ID

Gene Info:

Publications:

Chau I et al., 2006, Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials., Br J Cancer

Berna MJ et al., 2007, Role of CCK/gastrin receptors in gastrointestinal/metabolic diseases and results of human studies using gastrin/CCK receptor agonists/antagonists in these diseases., Curr Top Med Chem

NCI: CCKBR

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Håkanson et al., 1999, CCK2 receptor antagonists: pharmacological tools to study the gastrin-ECL cell-parietal cell axis., Regul. Pept.

Bock et al., 1994, Selective non-peptide ligands for an accommodating peptide receptor. Imidazobenzodiazepines as potent cholecystokinin type B receptor antagonists., Bioorg. Med. Chem.

Costall et al., 1991, Anxiolytic effects of CCK-B antagonists., Neuropeptides

DTC: CCKBR

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Harikumar KG et al., 2010, Modulation of cell surface expression of nonactivated cholecystokinin receptors using bivalent ligand-induced internalization., J Med Chem

Scott et al., 2012, Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017)., J. Med. Chem.

HingoraniCasas: ENSG00000110148
- Version: 31-May-2017
Alternate Names:

ENSG00000110148 Gene Symbol

CCKBR Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

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

CCKRB GENE_SYMBOL

CCKBR GENE_SYMBOL

Gastrin/cholecystokinin type B receptor UNIPROT

Gene Info:

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

887 Gene ID

CCK-B dGene Synonym

CCK2R dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

Mechanism of Interaction	Cholecystokinin B receptor antagonist
Direct Interaction	yes

Direct Interaction?	False
Endogenous Drug?	False
Specific Action of the Ligand	Antagonist

Endogenous Drug?	True
Specific Action of the Ligand	Full agonist

GASTRIN/CHOLECYSTOKININ TYPE B RECEPTOR (CCK-B RECEPTOR) (CCK-BR) (CHOLECYSTOKININ-2 RECEPTOR) (CCK2-R). [SOURCE:UNIPROT/SWISSPROT;ACC:P32239]	Description
CCKBR	Display Id
ENSG00000110148	Ensembl Gene Id

GASTRIN/CHOLECYSTOKININ TYPE B RECEPTOR	Uniprot Protein Name
P32239	Uniprot Accession
ENSG00000110148	Ensembl Gene Id

CCKBR	Gene Symbol
P32239	Uniprot Accession
ENSG00000110148	Ensembl Gene Id

1571	HUGO Gene ID
1571	HUGO Gene Symbol
cholecystokinin B receptor	HUGO Gene Name

CCKBR	DrugBank Gene Name
P32239	UniProt Accession
887	Entrez Gene Id

CCKRB	GENE_SYMBOL
CCKBR	GENE_SYMBOL
Gastrin/cholecystokinin type B receptor	UNIPROT

Trial Name	-
Novel drug target	Established target

CCKBR Gene Record

CCKBR 887 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 3004700 7491961 1732532 15157745 11752352 12073167

Sources: TEND TdgClinicalTrial TTD DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Cholecystokinin B receptor antagonist Direct Interaction yes

PMIDs: 17584143

Sources: TTD ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 20235611

Sources: DTC GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cholecystokinin B receptor antagonist Specific Action of the Ligand Antagonist

PMIDs: None found

Sources: TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cholecystokinin B receptor antagonist Specific Action of the Ligand Antagonist

PMIDs: None found

Sources: GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22691057

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10235629 7712133

Sources: NCI

Interaction Types & Directionality: agonist (activating)

Interaction Info: Endogenous Drug? True Specific Action of the Ligand Full agonist

PMIDs: None found

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 14602717 8876029

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 1679211

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
3004700 7491961 1732532 15157745 11752352 12073167

Sources:
TEND TdgClinicalTrial TTD DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Cholecystokinin B receptor antagonist

Direct Interaction yes

PMIDs:
17584143

Sources:
TTD ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
20235611

Sources:
DTC GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cholecystokinin B receptor antagonist

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cholecystokinin B receptor antagonist

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
22691057

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
10235629 7712133

Sources:
NCI

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? True

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
14602717 8876029

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
1679211

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
8771563

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
20732371

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
20732371

Sources:
PharmGKB

Alternate Names:

CCKBR Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Alternate Names:

GASTRIN/CHOLECYSTOKININ TYPE B RECEPTOR (CCK-B RECEPTOR) (CCK-BR) (CHOLECYSTOKININ-2 RECEPTOR) (CCK2-R). [SOURCE:UNIPROT/SWISSPROT;ACC:P32239] Description

CCKBR Display Id

ENSG00000110148 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Alternate Names:

GASTRIN/CHOLECYSTOKININ TYPE B RECEPTOR Uniprot Protein Name

P32239 Uniprot Accession

ENSG00000110148 Ensembl Gene Id