CCKAR

Summary

CCKAR (cholecystokinin A receptor, HGNC:1570) is a protein-coding gene on chromosome 4p15.2, encoding Cholecystokinin receptor type A (P32238). Receptor for cholecystokinin.

This gene encodes a G-protein coupled receptor that binds non-sulfated members of the cholecystokinin (CCK) family of peptide hormones. This receptor is a major physiologic mediator of pancreatic enzyme secretion and smooth muscle contraction of the gallbladder and stomach. In the central and peripheral nervous system this receptor regulates satiety and the release of beta-endorphin and dopamine.

Source: NCBI Gene 886 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 63 total
• Druggable target: yes — 42 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000730

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:1570
Approved symbol	CCKAR
Name	cholecystokinin A receptor
Location	4p15.2
Locus type	gene with protein product
Status	Approved
Aliases	CCK1R, CCK-AR, CCK-1R
Ensembl gene	ENSG00000163394
Ensembl biotype	protein_coding
OMIM	118444
Entrez	886

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000295589

RefSeq mRNA: 1 — MANE Select: NM_000730 NM_000730

CCDS: CCDS3438

Canonical transcript exons

ENST00000295589 — 5 exons

Exon	Start	End
ENSE00001074093	26490156	26490484
ENSE00001074095	26481396	26482170
ENSE00001122426	26483156	26483283
ENSE00001122433	26485637	26485898
ENSE00001122440	26489233	26489484

Expression profiles

Bgee: expression breadth broad, 56 present calls, max score 91.02.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 1.0413 / max 71.3579, expressed in 147 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
51716	0.6712	121
51714	0.2211	98
51715	0.0924	30
51718	0.0345	19
51717	0.0222	9

Top tissues by expression

270 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
gall bladder	UBERON:0002110	91.02	gold quality
type B pancreatic cell	CL:0000169	82.28	gold quality
olfactory bulb	UBERON:0002264	82.07	gold quality
endometrium epithelium	UBERON:0004811	79.38	gold quality
Brodmann (1909) area 10	UBERON:0013541	79.23	gold quality
body of stomach	UBERON:0001161	76.91	gold quality
stomach	UBERON:0000945	75.23	gold quality
tongue squamous epithelium	UBERON:0006919	71.62	gold quality
fundus of stomach	UBERON:0001160	68.71	gold quality
vastus lateralis	UBERON:0001379	67.98	gold quality
quadriceps femoris	UBERON:0001377	67.58	gold quality
frontal pole	UBERON:0002795	66.99	gold quality
paraflocculus	UBERON:0005351	66.65	gold quality
middle frontal gyrus	UBERON:0002702	66.61	gold quality
hair follicle	UBERON:0002073	64.58	gold quality
gingival epithelium	UBERON:0001949	63.07	gold quality
cerebellar vermis	UBERON:0004720	62.58	gold quality
triceps brachii	UBERON:0001509	62.15	gold quality
epithelial cell of pancreas	CL:0000083	62.10	gold quality
gluteal muscle	UBERON:0002000	62.07	gold quality
thymus	UBERON:0002370	61.39	gold quality
nasal cavity epithelium	UBERON:0005384	61.24	gold quality
gingiva	UBERON:0001828	60.55	gold quality
secondary oocyte	CL:0000655	60.46	gold quality
diaphragm	UBERON:0001103	60.25	gold quality
germinal epithelium of ovary	UBERON:0001304	59.67	gold quality
mucosa of urinary bladder	UBERON:0001259	59.52	gold quality
epithelium of esophagus	UBERON:0001976	59.25	gold quality
squamous epithelium	UBERON:0006914	59.25	gold quality
orbitofrontal cortex	UBERON:0004167	59.23	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	1.63

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

12 targeting CCKAR, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-3667-3P	99.99	67.17	1636
HSA-MIR-1236-3P	99.94	68.04	1695
HSA-MIR-3156-3P	99.76	66.72	939
HSA-MIR-3659	99.70	67.97	694
HSA-MIR-6128	99.33	67.83	1581
HSA-MIR-320A-5P	98.88	66.75	1248
HSA-MIR-4297	98.77	66.95	2013
HSA-MIR-6868-3P	98.63	69.64	2259
HSA-MIR-1237-3P	98.55	67.65	1423
HSA-MIR-5581-5P	97.91	66.50	965
HSA-MIR-203B-3P	97.82	66.27	979
HSA-MIR-874-5P	96.93	63.92	1014

Literature-anchored findings (GeneRIF, showing 39)

• Significant association between polymorphism at the -85 locus of the CCKAR gene in patients with hallucination, especially patients with hallucination in delirium tremens. (PMID:12198366)
• in Chinese, visual hallucinations in Parkinson’s disease are associated with cholecystokinin -45C>T polymorphism, and this association was still observed in the presence of the cholecystokinin-A receptor TC/CC genotype (PMID:12777967)
• the presence of CCK receptors in human ductal pancreatic tumor samples is mainly due to CCK2 expression in residual pancreatic islets and CCK1 in pancreatic nerves. (PMID:12851875)
• heterodimerization of type A and B cholecystokinin receptors forms a powerful signaling unit with potential clinical significance in promoting cell growth (PMID:14534299)
• In this review, both localization and functional studies suggest that the motor effects of cholecystokinin are mediated by CCK1/CCKA receptors in humans. (PMID:15100163)
• CCK-AR gene polymorphism may be involved in the neurobiology of panic disorder. (PMID:15108185)
• CCK-AR gene is suggested to predispose persons to schizophrenia. (PMID:15363473)
• analysis of partial and full agonism mediated by the human cholecystokinin-1 receptor (PMID:15632187)
• Finds significant differences in intelligence for Cholecystokinin A receptor gene promoter polymorphisms A-81G and G-128T in community-living Japanese. (PMID:15723764)
• the deficiency of CCK-R may be a key point leading to the impairment of gallbladder motor function and the pathogenesis of cholesterol gallstone formation (PMID:15786550)
• possible role of the CCK-AR gene in the vulnerability to schizophrenia in patients with auditory hallucinations (PMID:17413443)
• No evidence for the association between the CCK-AR gene and schizophrenia in the Japanese population. (PMID:17413452)
• CCK-A receptor agonist, GI181771X, did not reduce body in obese patients, suggesting that CCK-A by itself does not have a central role in long-term energy balance. (PMID:17597711)
• Responses of human esophageal sphincter sling and clasp fibers to cholecystokinin (CCK) and gastrin through CCK-A and -B receptors are reported. (PMID:18444993)
• Report effects of cholecystokinin-58 on type 1 cholecystokinin receptor function and regulation. (PMID:18776046)
• LPS can up-regulate the expression of CCK-AR and CCK-BR mRNA in vascular endothelial cells. (PMID:19751565)
• an intron 1 polymorphism in the cholecystokinin A receptor gene is associated with schizophrenia in males (PMID:19753663)
• a 2-marker haplotype (rs1800855/rs1800857) in the CCKAR gene protected women against PD (P=0.004). In addition, we found two novel rare missense variations in the CCKBR gene (Lys329Asn and Pro446Leu) in two and one patient, respectively (PMID:20023595)
• Impaired muscle contraction in gallbladders with cholesterol stones is due to high caveolar levels of cholesterol that inhibits CAV-3 generation; cholesterol increases the caveolar sequestration of CAV-3 and CCK-1R. (PMID:20558763)
• An association is not found between cholecystokinin A receptor polymorphisms and antipsychotic induced weight gain in schizophrenia patients. (PMID:20732371)
• Data indicate that the Homo-Phe derivative 2 (VL-0797) enhanced 12-fold the affinity for the rat CCK(1)-R affinity and 15-fold for the human CCK(1)-R relative to the reference compound 12 (VL-0395). (PMID:21728335)
• CCKAR expression was significantly increased in gallbladder cancer compared to gallstone disease. (PMID:21813391)
• data may suggest that the TM3 CRAC cholesterol-binding motif could be responsible for the cholesterol sensitivity of the CCK1R. (PMID:22021636)
• Data suggest that CCK-1R expression is up-regulated in kidney tubules (but not in glomeruli) in patients with diabetic nephropathy; increased expression of CCK-1R in tubules appears to be biomarker of severity of proteinuria in these patients. (PMID:22396142)
• The results showed that three individual haplotypes of CCKAR were strongly associated with increased risk of schizophrenia. (PMID:22825913)
• A significant association of the cholecystokinin-A receptor (CCKAR) gene variation rs1800857 and language lateralization, is reported. (PMID:23341962)
• The findings suggest that variants in the CCKAR gene may influence the risk of gallbladder cancer in women. (PMID:23701593)
• Y140A mutation within a cholesterol-binding motif results in ligand binding and activity characteristics similar to wild type CCK1R. in a high cholesterol environment (PMID:24825903)
• CCK binding modulates the contractile function of the lower esophageal sphincter through differential binding to the CCK-A receptor on the sling and clasp fibers (PMID:24914377)
• Age related differential expression of CCKAR in GBC may suggest two possible variants of the disease in this endemic belt. (PMID:25025063)
• There is functional synergy between cholecystokinin receptors CCKAR and CCKBR in mammalian brain development. (PMID:25875176)
• CCK1R may play a role differing from CCK2R in colon carcinogenesis, nuclear CCK1R represents a potential biomarker for poor prognosis. (PMID:26508021)
• CCK-AR polymorphism is protective against functional dyspepsia. (PMID:26551933)
• The neurotransmitter cholecystokinin (CCK), along with its receptors, CCKAR and CCKBR, have been previously associated with psychiatric disorders, suggesting that variants near these genes may play a role in the pre-pulse/startle response in this cohort (PMID:26608796)
• Our study showed significantly higher expression of CCKAR and down regulation of CCKBR in pancreatic cancer as compared to control while CCKBR/GR was detected in majority of stomach cancer samples. Thus, our study suggests that CCK and Gs receptors may have diagnostic and therapeutic implications. (PMID:27072272)
• Study shows downregulation of CCKAR gene expression in A1/A1 genotype of gallstone disease patients as compared with control with significant variation in its expression pattern in relation to polymorphism. (PMID:27287528)
• Photodynamic Activation of Cholecystokinin 1 Receptor with Different Genetically Encoded Protein Photosensitizers and from Varied Subcellular Sites. (PMID:33050050)
• Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins provide insight into mechanisms of G protein selectivity. (PMID:34086670)
• Cholesterol-dependent dynamic changes in the conformation of the type 1 cholecystokinin receptor affect ligand binding and G protein coupling. (PMID:39083706)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	CCKAR	ENSDARG00000052089
mus_musculus	Cckar	ENSMUSG00000029193
rattus_norvegicus	Cckar	ENSRNOG00000043124
drosophila_melanogaster	CCKLR-17D3	FBGN0030954
drosophila_melanogaster	CCKLR-17D1	FBGN0259231

Paralogs (16): NPFFR2 (ENSG00000056291), GNRHR (ENSG00000109163), CCKBR (ENSG00000110148), HCRTR1 (ENSG00000121764), AVPR2 (ENSG00000126895), GALR3 (ENSG00000128310), HCRTR2 (ENSG00000137252), NPFFR1 (ENSG00000148734), AVPR1A (ENSG00000166148), GALR1 (ENSG00000166573), GPR22 (ENSG00000172209), GPR150 (ENSG00000178015), OXTR (ENSG00000180914), FFAR4 (ENSG00000186188), QRFPR (ENSG00000186867), AVPR1B (ENSG00000198049)

Protein

Protein identifiers

Cholecystokinin receptor type A — P32238 (reviewed: P32238)

Alternative names: Cholecystokinin-1 receptor

All UniProt accessions (1): P32238

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for cholecystokinin. Mediates pancreatic growth and enzyme secretion, smooth muscle contraction of the gall bladder and stomach. Has a 1000-fold higher affinity for CCK rather than for gastrin. It modulates feeding and dopamine-induced behavior in the central and peripheral nervous system. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.

Subcellular location. Cell membrane.

Similarity. Belongs to the G-protein coupled receptor 1 family.

RefSeq proteins (1): NP_000721* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000596	Cholcy_rcpt_A	Family
IPR009126	Cholcskin_rcpt	Family
IPR015276	CholecystokininA_recpt_N	Domain
IPR017452	GPCR_Rhodpsn_7TM	Domain
IPR036472	CholecystokininA_recpt_N_sf	Homologous_superfamily

Pfam: PF00001, PF09193

UniProt features (47 total): helix 15, topological domain 8, transmembrane region 7, strand 4, glycosylation site 3, turn 3, region of interest 2, disulfide bond 2, chain 1, compositionally biased region 1, lipid moiety-binding region 1

Structure

Experimental structures (PDB)

14 structures.

PDB	Method	Resolution (Å)
7MBX	ELECTRON MICROSCOPY	1.95
7MBY	ELECTRON MICROSCOPY	2.44
7F8Y	X-RAY DIFFRACTION	2.5
9BKK	ELECTRON MICROSCOPY	2.51
9BKJ	ELECTRON MICROSCOPY	2.59
7F8U	X-RAY DIFFRACTION	2.8
7EZM	ELECTRON MICROSCOPY	2.9
7F8X	X-RAY DIFFRACTION	3
7XOV	ELECTRON MICROSCOPY	3
7EZK	ELECTRON MICROSCOPY	3.1
7EZH	ELECTRON MICROSCOPY	3.2
7XOU	ELECTRON MICROSCOPY	3.2
1D6G	SOLUTION NMR
1HZN	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P32238-F1	78.36	0.54

Antibody-complex structures (SAbDab): 5 — 7EZH, 7EZM, 7MBX, 7XOU, 7XOV

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (1): 387

Disulfide bonds (2): 18–29, 114–196

Glycosylation sites (3): 10, 24, 190

Function

Pathways and Gene Ontology

Reactome pathways

7 pathways

ID	Pathway
R-HSA-375276	Peptide ligand-binding receptors
R-HSA-416476	G alpha (q) signalling events
R-HSA-162582	Signal Transduction
R-HSA-372790	Signaling by GPCR
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)
R-HSA-388396	GPCR downstream signalling
R-HSA-500792	GPCR ligand binding

MSigDB gene sets: 124 (showing top): RNGTGGGC_UNKNOWN, MORF_FLT1, YAGI_AML_WITH_INV_16_TRANSLOCATION, MODULE_64, AREB6_03, GOBP_REGULATION_OF_HORMONE_LEVELS, GOBP_HORMONE_TRANSPORT, GOBP_NEUROGENESIS, GOBP_FOREBRAIN_DEVELOPMENT, GOBP_CELL_CELL_SIGNALING, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS, MODULE_379, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, SCHAEFFER_PROSTATE_DEVELOPMENT_48HR_DN

GO Biological Process (9): neuron migration (GO:0001764), G protein-coupled receptor signaling pathway (GO:0007186), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), axonogenesis (GO:0007409), forebrain development (GO:0030900), cellular response to hormone stimulus (GO:0032870), cholecystokinin signaling pathway (GO:0038188), regulation of hormone secretion (GO:0046883), signal transduction (GO:0007165)

GO Molecular Function (3): cholecystokinin receptor activity (GO:0004951), peptide hormone binding (GO:0017046), G protein-coupled receptor activity (GO:0004930)

GO Cellular Component (4): nucleoplasm (GO:0005654), cytosol (GO:0005829), plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-5 pathways:

Category	Pathways
Signaling by GPCR	2
Class A/1 (Rhodopsin-like receptors)	1
GPCR downstream signalling	1
Signal Transduction	1
GPCR ligand binding	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	3
cellular anatomical structure	3
cell migration	1
generation of neurons	1
G protein-coupled receptor activity	1
signal transduction	1
phospholipase C activator activity	1
cell morphogenesis involved in neuron differentiation	1
neuron projection morphogenesis	1
axon development	1
brain development	1
anatomical structure development	1
response to hormone	1
cellular response to chemical stimulus	1
cellular response to endogenous stimulus	1
regulation of cell communication	1
regulation of hormone levels	1
regulation of signaling	1
hormone secretion	1
regulation of secretion by cell	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
G protein-coupled peptide receptor activity	1
cholecystokinin signaling pathway	1
hormone binding	1
transmembrane signaling receptor activity	1
nuclear lumen	1
cytoplasm	1
membrane	1
cell periphery	1

Protein interactions and networks

STRING

1116 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CCKAR	CCK	P06307	999
CCKAR	GAST	P01350	952
CCKAR	PTK7	Q13308	950
CCKAR	CCL28	Q9NRJ3	950
CCKAR	PCDH7	O60245	787
CCKAR	STIM2	Q9P246	736
CCKAR	LEP	P41159	712
CCKAR	TBC1D1	Q86TI0	691
CCKAR	GCG	P01275	683
CCKAR	GLP1R	P43220	681
CCKAR	GIP	P09681	646
CCKAR	PYY	P10082	591
CCKAR	GCGR	P47871	565
CCKAR	NPY	P01303	556
CCKAR	GNAQ	P50148	537

IntAct

22 interactions, top by confidence:

A	B	Type	Score
	CCKAR	psi-mi:“MI:0915”(physical association)	0.400
CCKAR	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
RAMP1	CCKAR	psi-mi:“MI:0915”(physical association)	0.400
CCKAR	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	CCKAR	psi-mi:“MI:0915”(physical association)	0.400
CCKAR	RAMP3	psi-mi:“MI:0915”(physical association)	0.400
RAMP2	CCKAR	psi-mi:“MI:0915”(physical association)	0.400
CCKAR	PPP1R9B	psi-mi:“MI:0915”(physical association)	0.400

BioGRID (1): CCK (Protein-peptide)

ESM2 similar proteins: A5A4K9, A5A4L1, B2ZI34, F1MV99, O08725, O08786, O42329, O43193, O62709, O97772, P11616, P21451, P21729, P24053, P25099, P26684, P28088, P28190, P28646, P30542, P30550, P30551, P30872, P30873, P32238, P33534, P34970, P34975, P35342, P41144, P41145, P47745, P47751, P48302, P52500, P60893, P60894, P60895, Q2KIP6, Q49LX5

Diamond homologs: A0A287A2K5, C8YUV0, O00155, O02836, O08786, O15973, O18935, O19012, O19014, O19025, O19032, O19054, O19091, O62729, O77408, O77700, O77721, O77830, O97665, O97772, P04761, P08482, P0C5I1, P11229, P12657, P17200, P18089, P19328, P22270, P25021, P30545, P30551, P30552, P30553, P30796, P32211, P32238, P32239, P32302, P46627

SIGNOR signaling

13 interactions.

A	Effect	B	Mechanism
CCKAR	up-regulates	GNAQ	binding
CCKAR	“up-regulates activity”	GNAS	binding
CCKAR	“up-regulates activity”	GNAL	binding
CCKAR	“up-regulates activity”	GNAI1	binding
CCKAR	“up-regulates activity”	GNAI3	binding
CCKAR	“up-regulates activity”	GNAO1	binding
CCKAR	“up-regulates activity”	GNAQ	binding
CCKAR	“up-regulates activity”	GNA14	binding
CCKAR	“up-regulates activity”	GNA15	binding
Sincalide	“up-regulates activity”	CCKAR	“chemical activation”
CCK	up-regulates	CCKAR	binding
CCKAR	“up-regulates activity”	GNA13	binding
CCKAR	“up-regulates activity”	GNA12	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

63 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	58
Likely benign	2
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

738 predictions. Top by Δscore:

Variant	Effect	Δscore
4:26482455:T:A	donor_gain	1.0000
4:26483151:GTTA:G	donor_loss	1.0000
4:26483152:TTAC:T	donor_loss	1.0000
4:26483153:TA:T	donor_loss	1.0000
4:26483154:A:AG	donor_loss	1.0000
4:26483155:CCT:C	donor_loss	1.0000
4:26483246:C:CT	acceptor_gain	1.0000
4:26483246:C:T	acceptor_gain	1.0000
4:26483247:A:T	acceptor_gain	1.0000
4:26489228:CTTA:C	donor_loss	1.0000
4:26489229:TTACC:T	donor_loss	1.0000
4:26489230:TACCC:T	donor_loss	1.0000
4:26489231:A:AC	donor_gain	1.0000
4:26489231:AC:A	donor_gain	1.0000
4:26489231:ACC:A	donor_gain	1.0000
4:26489232:C:CT	donor_gain	1.0000
4:26489232:CC:C	donor_gain	1.0000
4:26489232:CCC:C	donor_gain	1.0000
4:26489232:CCCA:C	donor_gain	1.0000
4:26489232:CCCAT:C	donor_gain	1.0000
4:26489480:CCACT:C	acceptor_gain	1.0000
4:26489481:CACT:C	acceptor_gain	1.0000
4:26489481:CACTC:C	acceptor_gain	1.0000
4:26489482:ACT:A	acceptor_gain	1.0000
4:26489483:CT:C	acceptor_gain	1.0000
4:26489483:CTC:C	acceptor_gain	1.0000
4:26489484:TC:T	acceptor_loss	1.0000
4:26489484:TCT:T	acceptor_gain	1.0000
4:26489485:C:CC	acceptor_gain	1.0000
4:26489485:CTG:C	acceptor_loss	1.0000

AlphaMissense

2825 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
4:26485676:C:G	C196S	0.999
4:26485677:A:T	C196S	0.999
4:26485767:A:G	W166R	0.999
4:26485767:A:T	W166R	0.999
4:26489256:C:G	C114S	0.999
4:26489257:A:T	C114S	0.999
4:26489276:G:C	F107L	0.999
4:26489276:G:T	F107L	0.999
4:26489278:A:G	F107L	0.999
4:26489337:T:G	D87A	0.999
4:26489339:G:C	S86R	0.999
4:26489339:G:T	S86R	0.999
4:26489341:T:G	S86R	0.999
4:26481942:G:C	P328R	0.998
4:26481942:G:T	P328H	0.998
4:26481959:G:C	F322L	0.998
4:26481959:G:T	F322L	0.998
4:26481961:A:G	F322L	0.998
4:26485835:A:T	I143N	0.998
4:26485859:A:T	I135K	0.998
4:26485868:A:G	L132P	0.998
4:26485885:A:C	S126R	0.998
4:26485885:A:T	S126R	0.998
4:26485887:T:G	S126R	0.998
4:26489255:G:C	C114W	0.998
4:26489256:C:T	C114Y	0.998
4:26489257:A:G	C114R	0.998
4:26489337:T:A	D87V	0.998
4:26489337:T:C	D87G	0.998
4:26489420:G:C	N59K	0.998

dbSNP variants (sampled 300 via entrez): RS1000385406 (4:26488053 T>A,C), RS1000835809 (4:26483663 A>C), RS1000882061 (4:26488388 T>TC), RS10009085 (4:26489588 G>A), RS1001060462 (4:26489566 T>G), RS1001501549 (4:26480948 A>G), RS1001562145 (4:26487822 C>T), RS1001601027 (4:26481693 G>A,C,T), RS1001672970 (4:26486880 C>T), RS1002096753 (4:26488475 T>A), RS1002675756 (4:26485532 C>T), RS1002735407 (4:26486297 T>A), RS1002812015 (4:26485765 C>A), RS1003132020 (4:26492275 C>T), RS1003570187 (4:26491370 G>C)

Disease associations

OMIM: gene MIM:118444 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL1901 (SINGLE PROTEIN), CHEMBL2095185 (PROTEIN FAMILY), CHEMBL4523965 (SELECTIVITY GROUP)

Molecules with ChEMBL bioactivity

42 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 468,665 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1008	BEPRIDIL	4	11,776
CHEMBL1014	CANDESARTAN CILEXETIL	4	11,194
CHEMBL1017	TELMISARTAN	4	27,457
CHEMBL111	RIMONABANT	4	15,726
CHEMBL1121	SINCALIDE	4	27,601
CHEMBL1163	ATAZANAVIR	4	22,094
CHEMBL1173655	AFATINIB	4	15,144
CHEMBL1200515	DESERPIDINE	4	2,483
CHEMBL1201304	INDOCYANINE GREEN ACID FORM	4	7,044
CHEMBL1237021	LURASIDONE	4	2,517
CHEMBL1241951	LETERMOVIR	4	1,026
CHEMBL1401	NITAZOXANIDE	4	9,504
CHEMBL1423	PIMOZIDE	4	17,310
CHEMBL1617	RIFAXIMIN	4	13,380
CHEMBL163	RITONAVIR	4	53,773
CHEMBL178	DAUNORUBICIN	4	203,756
CHEMBL190461	CANNABIDIOL	4	26,379
CHEMBL2103737	HYDROXOCOBALAMIN	4
CHEMBL2103855	TELOTRISTAT	4	310
CHEMBL2105695	TELOTRISTAT ETHYL	4	191
CHEMBL2220442	FLUVASTATIN	4
CHEMBL222559	TIPRANAVIR	4
CHEMBL3353410	OSIMERTINIB	4
CHEMBL361812	RAMATROBAN	4
CHEMBL374478	RIFAMPIN	4
CHEMBL428647	PACLITAXEL	4
CHEMBL43	AMSACRINE	4
CHEMBL535	SUNITINIB	4
CHEMBL5416410	DASATINIB	4
CHEMBL553	ERLOTINIB	4

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Cholecystokinin receptors

Most potent curated ligand interactions (37 total), top 25:

Ligand	Action	Affinity	Parameter
ARL-15849	Full agonist	10.5	pKi
devazepide	Antagonist	9.72	pIC50
[3H]devazepide	Antagonist	9.7	pKd
T-0632	Antagonist	9.6	pIC50
pranazepide	Antagonist	9.4	pIC50
SR146131	Full agonist	9.3	pIC50
CCK-58	Full agonist	9.2	pIC50
[125I]DTyr-Gly-[(Nle28,31)CCK-26-33	Full agonist	9.0	pIC50
IQM-97423	Antagonist	9.0	pIC50
TP-680	Antagonist	8.9	pKi
PD-140548	Antagonist	8.6	pIC50
A-71623	Full agonist	8.4	pIC50
JMV180	Full agonist	8.3	pIC50
lintitript	Antagonist	8.3	pIC50
lorglumide	Antagonist	8.2	pIC50
JNJ-17156516	Antagonist	8.0	pKi
SC-50998	Antagonist	7.8	pIC50
GW-5823	Full agonist	7.6	pIC50
dexloxiglumide	Antagonist	7.5	pKi
CE-326597	Agonist	7.5	pIC50
Glaxo-11p	Full agonist	7.2	pIC50
YF-476	Antagonist	6.9	pIC50
YM-022	Antagonist	6.8	pKi
VL-0395	Antagonist	6.7	pIC50
L-365260	Antagonist	6.6	pIC50

Binding affinities (BindingDB)

16 measured of 21 human assays (21 total across all organisms); most potent 16 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
(3S)-3-[(2S)-2-[(2S)-2-{2-[(2S)-2-[(2S)-2-[(3S)-3-amino-3-formamidopropanoic acid]-3-[4-(sulfooxy)phenyl]propanamido]-4-(methylsulfanyl)butanamido]acetamido}-3-(1H-indol-3-yl)propanamido]-4-(methylsulfanyl)butanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid	KD	1.9 nM
3-[(R)-2-Amino-2-((S)-1-benzyl-2-carboxy-ethylcarbamoyl)-propyl]-indole-1-carboxylic acid adamantan-2-yl ester	KI	3 nM
(3S)-3-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]hexanamido]acetamido}-3-(1H-indol-3-yl)propanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid	KI	9.6 nM
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2	KI	98 nM
(3S)-3-[(2S)-2-[(2R)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid	KI	320 nM
CHEMBL227369	KI	372 nM
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2	KI	910 nM
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2	KI	1100 nM
CHEMBL374388	KI	1900 nM
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2	KI	2000 nM
{[2-(Adamantan-2-yloxycarbonylamino)-2-methyl-3-naphthalen-2-yl-propionyl]-phenethyl-amino}-acetic acid	KI	3010 nM
(3S)-3-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-[(3S)-3-amino-3-formamidopropanoic acid]-3-(4-hydroxyphenyl)propanamido]-3-phenylpropanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid	KI	3200 nM
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2	KI	3600 nM
(3S)-3-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid	KI	5100 nM
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2	KI	5700 nM
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2	KI	6500 nM

ChEMBL bioactivities

952 potent at pChembl≥5 of 1053 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	EC50	0.01	nM	CHEMBL1269257
11.00	IC50	0.01	nM	CHEMBL504114
10.89	EC50	0.013	nM	CHEMBL1269257
10.85	EC50	0.014	nM	CHEMBL156605
10.80	IC50	0.016	nM	CHEMBL509464
10.74	IC50	0.018	nM	CHEMBL450105
10.72	EC50	0.019	nM	CHEMBL156605
10.70	EC50	0.02	nM	CHEMBL105775
10.63	Ki	0.02344	nM	DEVAZEPIDE
10.60	EC50	0.02512	nM	CHEMBL423907
10.52	IC50	0.03	nM	CHEMBL509519
10.52	IC50	0.03	nM	CHEMBL505225
10.48	EC50	0.033	nM	CHEMBL504406
10.47	EC50	0.034	nM	CHEMBL498958
10.47	IC50	0.034	nM	CHEMBL1773877
10.41	EC50	0.039	nM	CHEMBL156605
10.41	IC50	0.039	nM	CHEMBL508004
10.40	EC50	0.04	nM	CHEMBL502974
10.40	IC50	0.04	nM	CHEMBL504861
10.39	IC50	0.04074	nM	CHEMBL4526455
10.39	IC50	0.041	nM	CHEMBL498958
10.37	IC50	0.04266	nM	CHEMBL4585323
10.36	EC50	0.04365	nM	SINCALIDE
10.35	IC50	0.04467	nM	CHEMBL423907
10.32	EC50	0.048	nM	CHEMBL498942
10.30	IC50	0.05012	nM	CHEMBL4525615
10.29	EC50	0.051	nM	CHEMBL105775
10.28	IC50	0.05248	nM	CHEMBL4440419
10.28	EC50	0.053	nM	CHEMBL509464
10.28	IC50	0.052	nM	CHEMBL468372
10.28	EC50	0.053	nM	CHEMBL510690
10.26	EC50	0.055	nM	CHEMBL504861
10.25	EC50	0.056	nM	CHEMBL504861
10.24	IC50	0.058	nM	CHEMBL504406
10.22	IC50	0.06026	nM	CHEMBL4514283
10.22	EC50	0.06026	nM	CHEMBL4464703
10.22	IC50	0.06	nM	CHEMBL504861
10.20	IC50	0.0631	nM	CHEMBL4440303
10.20	EC50	0.063	nM	CHEMBL1774043
10.19	IC50	0.06457	nM	CHEMBL4483457
10.19	EC50	0.065	nM	CHEMBL468372
10.19	EC50	0.065	nM	CHEMBL1773877
10.17	EC50	0.06761	nM	CHEMBL4453982
10.17	IC50	0.067	nM	CHEMBL451342
10.15	EC50	0.071	nM	CHEMBL504114
10.15	IC50	0.07	nM	CHEMBL510690
10.13	IC50	0.07413	nM	CHEMBL4583158
10.13	IC50	0.07413	nM	CHEMBL4441596
10.13	EC50	0.074	nM	CHEMBL507094
10.12	IC50	0.07586	nM	CHEMBL4563364

PubChem BioAssay actives

1038 with measured affinity, of 3267 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
2-[2,4-dioxo-5-phenyl-3-(phenylcarbamoylamino)-1,5-benzodiazepin-1-yl]-N-phenylacetamide	1198965: Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)	ec50	<0.0001	uM
(3R)-4-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-[[(2S)-2-[[2-(4-sulfooxyphenyl)acetyl]amino]hexanoyl]amino]acetyl]amino]propanoyl]amino]hexanoyl]-methylamino]-4-oxobutanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	<0.0001	uM
20-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-[4-(sulfomethyl)phenyl]propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-20-oxoicosanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	<0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-3-naphthalen-1-yl-1-oxopropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	<0.0001	uM
3-[(3R)-3-(acetamidomethyl)-4-[1-(3-ethoxyphenyl)-2-(2-fluoro-4-methylphenyl)imidazole-4-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acid	365389: Agonist activity at human CCK1 receptor	ec50	<0.0001	uM
2-[[(2S)-1-[1-(3-ethoxyphenyl)-2-(4-methylphenyl)imidazole-4-carbonyl]-4-quinolin-3-ylpiperazine-2-carbonyl]amino]acetic acid	365391: Inhibition of human CCK1 receptor	ic50	<0.0001	uM
3-[(3S)-4-[1-(3-ethoxyphenyl)-2-(2-fluoro-4-methylphenyl)imidazole-4-carbonyl]-3-(propan-2-ylcarbamoyl)piperazin-1-yl]naphthalene-1-carboxylic acid	365391: Inhibition of human CCK1 receptor	ic50	<0.0001	uM
3-[4-[1-(3-ethoxyphenyl)-2-(2-fluoro-4-methylphenyl)imidazole-4-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acid	365391: Inhibition of human CCK1 receptor	ic50	<0.0001	uM
3-[4-[1-(3-ethoxyphenyl)-2-(4-fluorophenyl)imidazole-4-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acid	342104: Agonist activity against human CCK1 receptor	ec50	<0.0001	uM
3-[4-[1-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-(4-fluorophenyl)imidazole-4-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acid	342106: Inhibition of human CCK1 receptor	ic50	<0.0001	uM
3-[4-[1-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-(2-fluoro-4-methylphenyl)imidazole-4-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acid	342106: Inhibition of human CCK1 receptor	ic50	<0.0001	uM
2-[2,4-dioxo-5-phenyl-3-(phenylcarbamoylamino)-1,5-benzodiazepin-1-yl]-N-(4-methoxyphenyl)-N-methylacetamide	1198965: Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)	ec50	<0.0001	uM
N-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamide	262761: Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line	ki	<0.0001	uM
3-[(3S)-3-(acetamidomethyl)-4-[1-(3-ethoxyphenyl)-2-(4-methylphenyl)imidazole-4-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acid	365389: Agonist activity at human CCK1 receptor	ec50	<0.0001	uM
3-[(3S)-4-[1-(3-ethoxyphenyl)-2-(4-methylphenyl)imidazole-4-carbonyl]-3-(propan-2-ylcarbamoyl)piperazin-1-yl]naphthalene-1-carboxylic acid	365391: Inhibition of human CCK1 receptor	ic50	<0.0001	uM
3-[(3S)-3-(carboxymethoxymethyl)-4-[1-(3-ethoxyphenyl)-2-(2-fluoro-4-methylphenyl)imidazole-4-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acid	365389: Agonist activity at human CCK1 receptor	ec50	<0.0001	uM
2-[[(2R)-1-[1-(3-ethoxyphenyl)-2-(4-methylphenyl)imidazole-4-carbonyl]-4-quinolin-3-ylpiperazin-2-yl]methoxy]acetic acid	365391: Inhibition of human CCK1 receptor	ic50	<0.0001	uM
3-[[(3S)-2,4-dioxo-1-[2-oxo-2-(N-propan-2-ylanilino)ethyl]-5-phenyl-1,5-benzodiazepin-3-yl]carbamoylamino]benzoic acid	1198961: Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.01 nM (Rvb = 7 to 14 pM)	ec50	<0.0001	uM
3-[4-[5-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-(2-fluoro-4-methylphenyl)pyrimidine-2-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acid	595922: Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting	ic50	<0.0001	uM
Sincalide	1572003: Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay	ec50	<0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-[4-(sulfomethyl)phenyl]propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-6-amino-1-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-[4-(sulfomethyl)phenyl]propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-1-oxohexan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-3-naphthalen-1-yl-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572003: Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay	ec50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[3-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[3-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethylamino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-naphthalen-1-yl-1-oxopropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-[4-(sulfomethyl)phenyl]propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572003: Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay	ec50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(4R)-5-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-[[2-(4-hydroxyphenyl)acetyl]amino]-5-oxopentyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572003: Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay	ec50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572003: Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay	ec50	0.0001	uM
18-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]amino]-6-[(2-methylphenyl)carbamoylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572003: Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay	ec50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-5-amino-1-[[(2R)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1,5-dioxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-[4-(sulfomethyl)phenyl]propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572003: Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay	ec50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-3-(4-sulfooxyphenyl)propanoyl]amino]-6-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-2-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572003: Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay	ec50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(1S)-3-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-[4-(sulfomethyl)phenyl]propan-2-yl]amino]-1-carboxy-3-oxopropyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-6-[(2-methylphenyl)carbamoylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572003: Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay	ec50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-naphthalen-1-yl-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-naphthalen-1-yl-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-carboxy-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-(4-sulfooxyphenyl)propan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	1572001: Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay	ic50	0.0001	uM
3-[4-[1-(3-ethoxyphenyl)-2-(4-methylphenyl)imidazole-4-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acid	342104: Agonist activity against human CCK1 receptor	ec50	0.0001	uM
2-[[(2S)-1-[1-(3-ethoxyphenyl)-2-(4-methylphenyl)imidazole-4-carbonyl]-4-quinolin-3-ylpiperazin-2-yl]methoxy]acetic acid	365389: Agonist activity at human CCK1 receptor	ec50	0.0001	uM
3-[4-[2-(2,4-difluorophenyl)-1-(3-ethoxyphenyl)imidazole-4-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acid	342104: Agonist activity against human CCK1 receptor	ec50	0.0001	uM
3-[4-[1-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-(4-methylphenyl)imidazole-4-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acid	342104: Agonist activity against human CCK1 receptor	ec50	0.0001	uM
3-[(3R)-3-(carboxymethoxymethyl)-4-[1-(3-ethoxyphenyl)-2-(4-methylphenyl)imidazole-4-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acid	365389: Agonist activity at human CCK1 receptor	ec50	0.0001	uM

CTD chemical–gene interactions

9 total (human), top 9 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, decreases expression	2
denatonium	decreases reaction, increases response to substance	1
Bolton Hunter-cholecystokinin nonapeptide	affects binding, decreases reaction	1
VL-0395	affects binding, decreases reaction	1
2-(2-((1H-indole-2-carbonyl)amino)benzoylamino)-4-phenylbutyric acid	affects binding, decreases reaction	1
Arsenic	affects methylation	1
Valproic Acid	increases methylation	1
Cyclosporine	increases methylation	1
Devazepide	decreases reaction, increases response to substance	1

ChEMBL screening assays

387 unique, capped per target: 310 binding, 75 functional, 1 admet, 1 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1004238	Binding	Inhibition of cholecystokinin A receptor	Recent natural products based drug development: a pharmaceutical industry perspective. — J Nat Prod
CHEMBL1030803	Functional	Agonist activity at human CCK1 receptor expressed in CHO cells assessed as stimulation of intracellular calcium response	Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors. — J Med Chem
CHEMBL4687882	ADMET	Displacement of [125I]CCK-8s from recombinant human CCK1 at 10 uM incubated for 60 mins by radiometric scintillation analysis relative to control	Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family. — Bioorg Med Chem

Cellosaurus cell lines

8 cell lines: 4 cancer cell line, 2 spontaneously immortalized cell line, 2 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_H411	CHO-K1/CCKA/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KW53	PathHunter CHO-K1 CCKAR beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_KZ37	PathHunter HEK 293 CCKAR beta-arrestin	Transformed cell line	Female
CVCL_KZ88	PathHunter U2OS CCKAR Activated GPCR Internalization	Cancer cell line	Female
CVCL_YK33	U2OS CCKAR calcium-Nomad	Cancer cell line	Female
CVCL_YK34	U2OS CCKAR DAG-Nomad	Cancer cell line	Female
CVCL_YK35	U2OS CCKAR HiTSeeker	Cancer cell line	Female
CVCL_ZK48	GeneBLAzer CCKAR-NFAT-bla HEK 293T	Transformed cell line	Female

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.