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Assay Detail

CHEMBL663474

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
112
Total Activities
112
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cholecystokinin receptor type A (CHEMBL2871)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.
Evans BE, Rittle KE, Bock MG, DiPardo RM, Freidinger RM, Whitter WL, Lundell GF, Veber DF, Anderson PS, Chang RS.
J Med Chem (1988) 31 : 2235 -2246
PubMed 2848124 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 112 6.70 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9506 DEVAZEPIDE 2.0 1 10.10
CHEMBL73946 1 9.12
CHEMBL1907850 1 9.10
CHEMBL1907848 1 9.10
CHEMBL39263 1 9.10
CHEMBL303227 1 8.89
CHEMBL73522 1 8.85
CHEMBL70456 1 8.85
CHEMBL71079 1 8.85
CHEMBL307661 1 8.82
CHEMBL306806 1 8.68
CHEMBL40211 1 8.64
CHEMBL1907852 1 8.60
CHEMBL2092869 1 8.54
CHEMBL1907851 1 8.46
CHEMBL306760 1 8.33
CHEMBL73885 1 8.33
CHEMBL308111 1 8.30
CHEMBL1907855 1 8.22
CHEMBL72300 1 8.22
CHEMBL72073 1 8.08
CHEMBL70856 1 8.05
CHEMBL1907841 1 7.96
CHEMBL443009 1 7.96
CHEMBL73561 1 7.82
CHEMBL1907846 1 7.82
CHEMBL70593 1 7.75
CHEMBL1907849 1 7.72
CHEMBL2092871 1 7.72
CHEMBL422951 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9506 DEVAZEPIDE IC50 = 0.08 nM 10.10
CHEMBL73946 IC50 = 0.75 nM 9.12
CHEMBL1907848 IC50 = 0.8 nM 9.10
CHEMBL39263 IC50 = 0.8 nM 9.10
CHEMBL1907850 IC50 = 0.8 nM 9.10
CHEMBL303227 IC50 = 1.3 nM 8.89
CHEMBL73522 IC50 = 1.4 nM 8.85
CHEMBL70456 IC50 = 1.4 nM 8.85
CHEMBL71079 IC50 = 1.4 nM 8.85
CHEMBL307661 IC50 = 1.5 nM 8.82
CHEMBL306806 IC50 = 2.1 nM 8.68
CHEMBL40211 IC50 = 2.3 nM 8.64
CHEMBL1907852 IC50 = 2.5 nM 8.60
CHEMBL2092869 IC50 = 2.9 nM 8.54
CHEMBL1907851 IC50 = 3.5 nM 8.46
CHEMBL306760 IC50 = 4.7 nM 8.33
CHEMBL73885 IC50 = 4.7 nM 8.33
CHEMBL308111 IC50 = 5.0 nM 8.30
CHEMBL72300 IC50 = 6.0 nM 8.22
CHEMBL1907855 IC50 = 6.0 nM 8.22
CHEMBL72073 IC50 = 8.3 nM 8.08
CHEMBL70856 IC50 = 9.0 nM 8.05
CHEMBL1907841 IC50 = 11.0 nM 7.96
CHEMBL443009 IC50 = 11.0 nM 7.96
CHEMBL1907846 IC50 = 15.0 nM 7.82
CHEMBL73561 IC50 = 15.0 nM 7.82
CHEMBL70593 IC50 = 18.0 nM 7.75
CHEMBL2092871 IC50 = 19.0 nM 7.72
CHEMBL1907849 IC50 = 19.0 nM 7.72
CHEMBL305951 IC50 = 20.0 nM 7.70
CHEMBL422951 IC50 = 20.0 nM 7.70
CHEMBL73510 IC50 = 21.0 nM 7.68
CHEMBL70549 IC50 = 22.0 nM 7.66
CHEMBL304768 IC50 = 28.0 nM 7.55
CHEMBL74515 IC50 = 29.0 nM 7.54
CHEMBL73621 IC50 = 32.0 nM 7.50
CHEMBL74580 IC50 = 41.0 nM 7.39
CHEMBL1907847 IC50 = 43.0 nM 7.37
CHEMBL2092868 IC50 = 49.0 nM 7.31
CHEMBL302825 IC50 = 66.0 nM 7.18
CHEMBL308414 IC50 = 71.0 nM 7.15
CHEMBL74066 IC50 = 71.0 nM 7.15
CHEMBL74125 IC50 = 81.0 nM 7.09
CHEMBL72550 IC50 = 87.0 nM 7.06
CHEMBL72599 IC50 = 96.0 nM 7.02
CHEMBL441445 IC50 = 100.0 nM 7.00
CHEMBL40668 IC50 = 110.0 nM 6.96
CHEMBL73272 IC50 = 110.0 nM 6.96
CHEMBL303724 IC50 = 110.0 nM 6.96
CHEMBL72667 IC50 = 120.0 nM 6.92