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Assay Detail

CHEMBL662287

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

Binding
Displacement of 0.2 nM [3H]pCCK-8 from guinea pig brain membranes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and binding affinities of cyclic and related linear analogues of CCK8 selective for central receptors.
Charpentier B, Dor A, Roy P, England P, Pham H, Durieux C, Roques BP.
J Med Chem (1989) 32 : 1184 -1190
PubMed 2724293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.86 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL384035 1 9.64
CHEMBL1121 SINCALIDE 4.0 1 9.55
CHEMBL264273 1 9.25
CHEMBL437661 1 8.33
CHEMBL2370588 1 8.19
CHEMBL267329 1 8.04
CHEMBL384731 1 7.56
CHEMBL266990 1 7.54
CHEMBL273880 1 7.33
CHEMBL216831 1 7.27
CHEMBL384618 1 6.52
CHEMBL440259 1 6.50
CHEMBL386304 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL384035 Ki = 0.23 nM 9.64
CHEMBL1121 SINCALIDE Ki = 0.28 nM 9.55
CHEMBL264273 Ki = 0.56 nM 9.25
CHEMBL437661 Ki = 4.7 nM 8.33
CHEMBL2370588 Ki = 6.43 nM 8.19
CHEMBL267329 Ki = 9.11 nM 8.04
CHEMBL384731 Ki = 27.5 nM 7.56
CHEMBL266990 Ki = 29.2 nM 7.54
CHEMBL273880 Ki = 47.3 nM 7.33
CHEMBL216831 Ki = 54.0 nM 7.27
CHEMBL384618 Ki = 301.0 nM 6.52
CHEMBL440259 Ki = 313.0 nM 6.50
CHEMBL386304 Ki = 334.0 nM 6.48