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Assay Detail

CHEMBL662568

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

Binding
Evaluated in vitro for its binding affinity towards 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

Synthesis and biological activity of CCK heptapeptide analogues. Effects of conformational constraints and standard modifications on receptor subtype selectivity, functional activity in vitro, and appetite suppression in vivo.
Holladay MW, Bennett MJ, Tufano MD, Lin CW, Asin KE, Witte DG, Miller TR, Bianchi BR, Nikkel AL, Bednarz L.
J Med Chem (1992) 35 : 2919 -2928
PubMed 1501220 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.53 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL412238 1 9.62
CHEMBL316949 1 9.30
CHEMBL316944 1 9.23
CHEMBL2310858 1 9.05
CHEMBL98631 1 8.96
CHEMBL439591 1 8.85
CHEMBL2310856 1 8.51
CHEMBL318010 1 8.47
CHEMBL98332 1 8.11
CHEMBL98720 1 7.82
CHEMBL316709 1 7.80
CHEMBL414793 1 7.62
CHEMBL408286 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL412238 IC50 = 0.24 nM 9.62
CHEMBL316949 IC50 = 0.5 nM 9.30
CHEMBL316944 IC50 = 0.59 nM 9.23
CHEMBL2310858 IC50 = 0.9 nM 9.05
CHEMBL98631 IC50 = 1.1 nM 8.96
CHEMBL439591 IC50 = 1.4 nM 8.85
CHEMBL2310856 IC50 = 3.1 nM 8.51
CHEMBL318010 IC50 = 3.4 nM 8.47
CHEMBL98332 IC50 = 7.7 nM 8.11
CHEMBL98720 IC50 = 15.0 nM 7.82
CHEMBL316709 IC50 = 16.0 nM 7.80
CHEMBL414793 IC50 = 24.0 nM 7.62
CHEMBL408286 IC50 = 32.0 nM 7.50