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Assay Detail

CHEMBL661925

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

Binding
Displacement of [125I]BH-CCK-8 from Cholecystokinin type B receptor of guinea pig cortex
13
Total Activities
13
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 CCK-tetrapeptide analogues as potent and selective CCK-A receptor agonists.
Shiosaki K, Lin CW, Kopecka H, Craig R, Wagenaar FL, Bianchi B, Miller T, Witte D, Nadzan AM.
J Med Chem (1990) 33 : 2950 -2952
PubMed 1700123 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.00 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1121 SINCALIDE 4.0 1 8.09
CHEMBL64605 1 7.60
CHEMBL216166 1 6.77
CHEMBL319814 1 5.96
CHEMBL262767 1 5.92
CHEMBL320868 1 5.82
CHEMBL319340 1 5.72
CHEMBL103485 1 5.72
CHEMBL98468 1 5.72
CHEMBL100609 1 5.42
CHEMBL156559 1 5.35
CHEMBL99786 1 5.31
CHEMBL328422 1 4.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1121 SINCALIDE IC50 = 8.2 nM 8.09
CHEMBL64605 IC50 = 25.0 nM 7.60
CHEMBL216166 IC50 = 170.0 nM 6.77
CHEMBL319814 IC50 = 1100.0 nM 5.96
CHEMBL262767 IC50 = 1200.0 nM 5.92
CHEMBL320868 IC50 = 1500.0 nM 5.82
CHEMBL319340 IC50 = 1900.0 nM 5.72
CHEMBL103485 IC50 = 1900.0 nM 5.72
CHEMBL98468 IC50 = 1900.0 nM 5.72
CHEMBL100609 IC50 = 3800.0 nM 5.42
CHEMBL156559 IC50 = 4500.0 nM 5.35
CHEMBL99786 IC50 = 4900.0 nM 5.31
CHEMBL328422 IC50 = 27000.0 nM 4.57