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Assay Detail

CHEMBL660355

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

Binding
In vitro inhibitory activity against Cholecystokinin type B receptor using [125I]BH-CCK-8S as radioligand in mouse cortical membranes
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Gastrin/cholecystokinin type B receptor (CHEMBL2854)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Non-peptide cholecystokinin-B/gastrin receptor antagonists based on bicyclic, heteroaromatic skeletons.
Kalindjian SB, Buck IM, Davies JM, Dunstone DJ, Hudson ML, Low CM, McDonald IM, Pether MJ, Steel KI, Tozer MJ, Vinter JG.
J Med Chem (1996) 39 : 1806 -1815
PubMed 8627604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.91 9.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415936 1 9.13
CHEMBL14557 1 8.96
CHEMBL299540 1 8.92
CHEMBL298521 1 8.91
CHEMBL296167 1 8.80
CHEMBL299387 1 8.41
CHEMBL53237 1 8.39
CHEMBL298551 1 8.35
CHEMBL24313 1 8.28
CHEMBL297480 1 8.27
CHEMBL301777 1 8.12
CHEMBL301810 1 7.88
CHEMBL280248 1 7.87
CHEMBL298861 1 7.82
CHEMBL300456 1 7.80
CHEMBL53129 1 6.47
CHEMBL301095 1 6.27
CHEMBL301740 1 6.05
CHEMBL52740 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415936 Ki = 0.7413 nM 9.13
CHEMBL14557 Ki = 1.096 nM 8.96
CHEMBL299540 Ki = 1.202 nM 8.92
CHEMBL298521 Ki = 1.23 nM 8.91
CHEMBL296167 Ki = 1.585 nM 8.80
CHEMBL299387 Ki = 3.89 nM 8.41
CHEMBL53237 Ki = 4.074 nM 8.39
CHEMBL298551 Ki = 4.467 nM 8.35
CHEMBL24313 Ki = 5.248 nM 8.28
CHEMBL297480 Ki = 5.37 nM 8.27
CHEMBL301777 Ki = 7.586 nM 8.12
CHEMBL301810 Ki = 13.18 nM 7.88
CHEMBL280248 Ki = 13.49 nM 7.87
CHEMBL298861 Ki = 15.14 nM 7.82
CHEMBL300456 Ki = 15.85 nM 7.80
CHEMBL53129 Ki = 338.84 nM 6.47
CHEMBL301095 Ki = 537.03 nM 6.27
CHEMBL301740 Ki = 891.25 nM 6.05
CHEMBL52740 Ki = 2884.03 nM 5.54