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Assay Detail

CHEMBL684537

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

Functional
Evaluated in vitro for maximal stimulatory activity for amylase release relative to CCK-8 in guinea pig tissue
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Cholecystokinin receptor (CHEMBL2095185)
Type PROTEIN FAMILY
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
EC50 9 8.15 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL316944 1 9.19
CHEMBL2310856 1 9.15
CHEMBL316949 1 9.00
CHEMBL318010 1 8.43
CHEMBL439591 1 8.43
CHEMBL412238 1 7.82
CHEMBL414793 1 7.30
CHEMBL98720 1 7.15
CHEMBL98631 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL316944 EC50 = 0.64 nM 9.19
CHEMBL2310856 EC50 = 0.7 nM 9.15
CHEMBL316949 EC50 = 0.99 nM 9.00
CHEMBL318010 EC50 = 3.7 nM 8.43
CHEMBL439591 EC50 = 3.7 nM 8.43
CHEMBL412238 EC50 = 15.0 nM 7.82
CHEMBL414793 EC50 = 50.0 nM 7.30
CHEMBL98720 EC50 = 71.0 nM 7.15
CHEMBL98631 EC50 = 140.0 nM 6.85