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Assay Detail

CHEMBL662466

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Functional
Inhibition of inositol phosphate production induced by Cholecystokinin type B receptor (0.5 nM)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Gastrin/cholecystokinin type B receptor (CHEMBL3508)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological properties of new constrained CCK-B antagonists: discrimination of two affinity states of the CCK-B receptor on transfected CHO cells.
Bellier B, McCort-Tranchepain I, Ducos B, Danascimento S, Meudal H, Noble F, Garbay C, Roques BP.
J Med Chem (1997) 40 : 3947 -3956
PubMed 9397175 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.04 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2062154 CI-988 1.0 1 7.52
CHEMBL338525 1 7.43
CHEMBL9387 L-365260 1 7.41
CHEMBL337934 1 7.26
CHEMBL337933 1 7.25
CHEMBL435404 1 7.14
CHEMBL338526 1 6.66
CHEMBL338300 1 6.41
CHEMBL406359 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2062154 CI-988 IC50 = 30.0 nM 7.52
CHEMBL338525 IC50 = 37.4 nM 7.43
CHEMBL9387 L-365260 IC50 = 39.0 nM 7.41
CHEMBL337934 IC50 = 55.5 nM 7.26
CHEMBL337933 IC50 = 55.8 nM 7.25
CHEMBL435404 IC50 = 72.0 nM 7.14
CHEMBL338526 IC50 = 217.0 nM 6.66
CHEMBL338300 IC50 = 389.0 nM 6.41
CHEMBL406359 IC50 = 507.0 nM 6.29