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Assay Detail

CHEMBL656248

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

Binding
Inhibition of binding of [125I]-CCK-8 to the cholecystokinin type B receptor
118
Total Activities
118
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Gastrin/cholecystokinin type B receptor (CHEMBL298)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of 1,4-benzodiazepine cholecystokinin type B antagonists.
Bock MG, DiPardo RM, Evans BE, Rittle KE, Whitter WL, Garsky VM, Gilbert KF, Leighton JL, Carson KL, Mellin EC.
J Med Chem (1993) 36 : 4276 -4292
PubMed 8277510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 118 7.37 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL137516 1 9.66
CHEMBL137726 1 9.62
CHEMBL313813 1 9.25
CHEMBL337574 1 9.22
CHEMBL342640 1 9.10
CHEMBL136966 1 9.00
CHEMBL38404 1 9.00
CHEMBL417521 1 8.92
CHEMBL2092976 1 8.85
CHEMBL445095 1 8.80
CHEMBL2448131 1 8.66
CHEMBL136038 1 8.57
CHEMBL137398 1 8.52
CHEMBL542967 1 8.46
CHEMBL337055 1 8.42
CHEMBL2111923 1 8.42
CHEMBL136608 1 8.42
CHEMBL135371 1 8.36
CHEMBL336765 1 8.32
CHEMBL137567 1 8.31
CHEMBL134340 1 8.30
CHEMBL135218 1 8.25
CHEMBL135538 1 8.24
CHEMBL422102 1 8.23
CHEMBL273919 1 8.23
CHEMBL337286 1 8.22
CHEMBL343767 1 8.22
CHEMBL33554 1 8.19
CHEMBL515268 1 8.16
CHEMBL132875 1 8.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL137516 IC50 = 0.22 nM 9.66
CHEMBL137726 IC50 = 0.24 nM 9.62
CHEMBL313813 IC50 = 0.56 nM 9.25
CHEMBL337574 IC50 = 0.6 nM 9.22
CHEMBL342640 IC50 = 0.8 nM 9.10
CHEMBL38404 IC50 = 1.0 nM 9.00
CHEMBL136966 IC50 = 1.0 nM 9.00
CHEMBL417521 IC50 = 1.2 nM 8.92
CHEMBL2092976 IC50 = 1.4 nM 8.85
CHEMBL445095 IC50 = 1.6 nM 8.80
CHEMBL2448131 IC50 = 2.2 nM 8.66
CHEMBL136038 IC50 = 2.7 nM 8.57
CHEMBL137398 IC50 = 3.0 nM 8.52
CHEMBL542967 IC50 = 3.5 nM 8.46
CHEMBL136608 IC50 = 3.8 nM 8.42
CHEMBL2111923 IC50 = 3.8 nM 8.42
CHEMBL337055 IC50 = 3.8 nM 8.42
CHEMBL135371 IC50 = 4.4 nM 8.36
CHEMBL336765 IC50 = 4.8 nM 8.32
CHEMBL137567 IC50 = 4.9 nM 8.31
CHEMBL134340 IC50 = 5.0 nM 8.30
CHEMBL135218 IC50 = 5.6 nM 8.25
CHEMBL135538 IC50 = 5.7 nM 8.24
CHEMBL273919 IC50 = 5.9 nM 8.23
CHEMBL422102 IC50 = 5.9 nM 8.23
CHEMBL343767 IC50 = 6.0 nM 8.22
CHEMBL337286 IC50 = 6.0 nM 8.22
CHEMBL33554 IC50 = 6.5 nM 8.19
CHEMBL515268 IC50 = 6.9 nM 8.16
CHEMBL132875 IC50 = 7.2 nM 8.14
CHEMBL2111924 IC50 = 7.5 nM 8.12
CHEMBL9449 IC50 = 8.0 nM 8.10
CHEMBL137043 IC50 = 7.9 nM 8.10
CHEMBL9387 L-365260 IC50 = 8.5 nM 8.07
CHEMBL136412 IC50 = 9.7 nM 8.01
CHEMBL137066 IC50 = 9.8 nM 8.01
CHEMBL136975 IC50 = 9.7 nM 8.01
CHEMBL137779 IC50 = 9.7 nM 8.01
CHEMBL334592 IC50 = 11.0 nM 7.96
CHEMBL337065 IC50 = 11.0 nM 7.96
CHEMBL1907927 IC50 = 13.0 nM 7.89
CHEMBL2112753 IC50 = 14.7 nM 7.83
CHEMBL2112751 IC50 = 19.0 nM 7.72
CHEMBL169661 IC50 = 19.6 nM 7.71
CHEMBL136436 IC50 = 22.0 nM 7.66
CHEMBL135433 IC50 = 22.0 nM 7.66
CHEMBL424076 IC50 = 22.0 nM 7.66
CHEMBL135447 IC50 = 26.0 nM 7.58
CHEMBL337733 IC50 = 26.0 nM 7.58
CHEMBL135289 IC50 = 26.0 nM 7.58