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Assay Detail

CHEMBL856757

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

Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cholecystokinin receptor type A (CHEMBL3501)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Structure-based design and pharmacological properties of potent selective and systemically active CCK-B peptidomimetics
Roques BP, Corringer P, Derrien M, Dauge V, Durieux C
Bioorg Med Chem Lett (1993) 3 : 847 -850
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.72 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1121 SINCALIDE 4.0 1 9.19
CHEMBL262894 1 7.21
CHEMBL428666 1 7.11
CHEMBL436722 1 6.00
CHEMBL412917 1 5.96
CHEMBL353862 1 5.96
CHEMBL171594 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1121 SINCALIDE Ki = 0.64 nM 9.19
CHEMBL262894 Ki = 62.0 nM 7.21
CHEMBL428666 Ki = 78.0 nM 7.11
CHEMBL436722 Ki = 1000.0 nM 6.00
CHEMBL412917 Ki = 1100.0 nM 5.96
CHEMBL353862 Ki = 1100.0 nM 5.96
CHEMBL171594 Ki = 2400.0 nM 5.62