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Assay Detail

CHEMBL661740

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

Binding
In vitro for binding affinity against human cholecystokinin type A receptor.
27
Total Activities
27
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 (CHEMBL1901)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
Henke BR, Aquino CJ, Birkemo LS, Croom DK, Dougherty RW, Ervin GN, Grizzle MK, Hirst GC, James MK, Johnson MF, Queen KL, Sherrill RG, Sugg EE, Suh EM, Szewczyk JW, Unwalla RJ, Yingling J, Willson TM.
J Med Chem (1997) 40 : 2706 -2725
PubMed 9276016 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.23 8.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1121 SINCALIDE 4.0 1 8.88
CHEMBL316164 1 8.08
CHEMBL88602 1 7.97
CHEMBL88629 1 7.88
CHEMBL328285 1 7.86
CHEMBL327815 1 7.84
CHEMBL327849 1 7.77
CHEMBL328586 1 7.76
CHEMBL327909 1 7.75
CHEMBL406790 1 7.68
CHEMBL293226 1 7.64
CHEMBL90697 1 7.53
CHEMBL316104 1 7.41
CHEMBL310466 1 7.37
CHEMBL94005 1 7.37
CHEMBL88545 1 7.06
CHEMBL91986 1 7.05
CHEMBL327656 1 6.95
CHEMBL316077 1 6.89
CHEMBL330521 1 6.86
CHEMBL89953 1 6.51
CHEMBL316106 1 6.45
CHEMBL92586 1 6.32
CHEMBL330566 1 6.28
CHEMBL327552 1 6.18
CHEMBL431451 1 6.05
CHEMBL329407 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1121 SINCALIDE IC50 = 1.318 nM 8.88
CHEMBL316164 IC50 = 8.318 nM 8.08
CHEMBL88602 IC50 = 10.81 nM 7.97
CHEMBL88629 IC50 = 13.18 nM 7.88
CHEMBL328285 IC50 = 13.8 nM 7.86
CHEMBL327815 IC50 = 14.45 nM 7.84
CHEMBL327849 IC50 = 16.98 nM 7.77
CHEMBL328586 IC50 = 17.38 nM 7.76
CHEMBL327909 IC50 = 17.78 nM 7.75
CHEMBL406790 IC50 = 20.89 nM 7.68
CHEMBL293226 IC50 = 22.91 nM 7.64
CHEMBL90697 IC50 = 29.51 nM 7.53
CHEMBL316104 IC50 = 38.9 nM 7.41
CHEMBL310466 IC50 = 42.66 nM 7.37
CHEMBL94005 IC50 = 42.66 nM 7.37
CHEMBL88545 IC50 = 87.1 nM 7.06
CHEMBL91986 IC50 = 89.13 nM 7.05
CHEMBL327656 IC50 = 112.2 nM 6.95
CHEMBL316077 IC50 = 128.82 nM 6.89
CHEMBL330521 IC50 = 138.04 nM 6.86
CHEMBL89953 IC50 = 309.03 nM 6.51
CHEMBL316106 IC50 = 354.81 nM 6.45
CHEMBL92586 IC50 = 478.63 nM 6.32
CHEMBL330566 IC50 = 524.81 nM 6.28
CHEMBL327552 IC50 = 660.69 nM 6.18
CHEMBL431451 IC50 = 891.25 nM 6.05
CHEMBL329407 IC50 = 1584.89 nM 5.80