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Assay Detail

CHEMBL662399

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

Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreas
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cholecystokinin receptor type A (CHEMBL2871)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel glutamic acid derived cholecystokinin receptor ligands.
Freidinger RM, Whitter WL, Gould NP, Holloway MK, Chang RS, Lotti VJ.
J Med Chem (1990) 33 : 591 -595
PubMed 2299627 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.84 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9506 DEVAZEPIDE 2.0 1 10.10
CHEMBL157658 1 8.35
CHEMBL158362 1 8.12
CHEMBL24938 LORGLUMIDE 2.0 1 7.75
CHEMBL422873 1 7.23
CHEMBL155017 1 6.92
CHEMBL348168 1 6.85
CHEMBL346070 1 6.77
CHEMBL158078 1 6.70
CHEMBL9387 L-365260 1 6.55
CHEMBL157722 1 6.27
CHEMBL346784 1 6.17
CHEMBL155406 1 6.09
CHEMBL422701 1 5.96
CHEMBL346361 1 5.92
CHEMBL156415 1 5.43
CHEMBL156814 1 5.03
CHEMBL316561 PROGLUMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9506 DEVAZEPIDE IC50 = 0.08 nM 10.10
CHEMBL157658 IC50 = 4.5 nM 8.35
CHEMBL158362 IC50 = 7.6 nM 8.12
CHEMBL24938 LORGLUMIDE IC50 = 18.0 nM 7.75
CHEMBL422873 IC50 = 59.0 nM 7.23
CHEMBL155017 IC50 = 120.0 nM 6.92
CHEMBL348168 IC50 = 140.0 nM 6.85
CHEMBL346070 IC50 = 170.0 nM 6.77
CHEMBL158078 IC50 = 200.0 nM 6.70
CHEMBL9387 L-365260 IC50 = 280.0 nM 6.55
CHEMBL157722 IC50 = 540.0 nM 6.27
CHEMBL346784 IC50 = 680.0 nM 6.17
CHEMBL155406 IC50 = 810.0 nM 6.09
CHEMBL422701 IC50 = 1100.0 nM 5.96
CHEMBL346361 IC50 = 1200.0 nM 5.92
CHEMBL156415 IC50 = 3700.0 nM 5.43
CHEMBL156814 IC50 = 9300.0 nM 5.03
CHEMBL316561 PROGLUMIDE IC50 = 250000.0 nM -