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Assay Detail

CHEMBL936346

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Binding
Binding affinity to human CCK1 receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholecystokinin receptor type A (CHEMBL1901)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Achiral, selective CCK2 receptor antagonists based on a 1,3,5-benzotriazepine-2,4-dione template.
Spencer J, Gaffen J, Griffin E, Harper EA, Linney ID, McDonald IM, Roberts SP, Shaxted ME, Adatia T, Bashall A.
Bioorg Med Chem (2008) 16 : 2974 -2983
PubMed 18289857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.77 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL324547 NETAZEPIDE 2.0 1 7.50
CHEMBL321761 1 7.30
CHEMBL320141 1 7.10
CHEMBL147186 1 6.90
CHEMBL317181 1 6.80
CHEMBL205455 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL324547 NETAZEPIDE Ki = 31.62 nM 7.50
CHEMBL321761 Ki = 50.12 nM 7.30
CHEMBL320141 Ki = 79.43 nM 7.10
CHEMBL147186 Ki = 125.89 nM 6.90
CHEMBL317181 Ki = 158.49 nM 6.80
CHEMBL205455 Ki = 10000.0 nM 5.00