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Assay Detail

CHEMBL663097

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

Binding
Inhibition of binding of [125I]gastrin to Cholecystokinin type B receptor from guinea pig gastric glands
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Stomach
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Gastrin/cholecystokinin type B receptor (CHEMBL298)
Type SINGLE PROTEIN
Organism Homo sapiens

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 5.79 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9387 L-365260 1 8.96
CHEMBL9506 DEVAZEPIDE 2.0 1 6.77
CHEMBL158362 1 6.77
CHEMBL155017 1 6.72
CHEMBL157658 1 6.51
CHEMBL346784 1 6.37
CHEMBL348168 1 6.16
CHEMBL346070 1 6.07
CHEMBL24938 LORGLUMIDE 2.0 1 5.72
CHEMBL422873 1 5.39
CHEMBL346361 1 5.35
CHEMBL155406 1 5.16
CHEMBL157722 1 4.89
CHEMBL156415 1 4.77
CHEMBL422701 1 4.41
CHEMBL156814 1 4.36
CHEMBL158078 1 4.00
CHEMBL316561 PROGLUMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9387 L-365260 IC50 = 1.1 nM 8.96
CHEMBL9506 DEVAZEPIDE IC50 = 170.0 nM 6.77
CHEMBL158362 IC50 = 170.0 nM 6.77
CHEMBL155017 IC50 = 190.0 nM 6.72
CHEMBL157658 IC50 = 310.0 nM 6.51
CHEMBL346784 IC50 = 430.0 nM 6.37
CHEMBL348168 IC50 = 700.0 nM 6.16
CHEMBL346070 IC50 = 860.0 nM 6.07
CHEMBL24938 LORGLUMIDE IC50 = 1900.0 nM 5.72
CHEMBL422873 IC50 = 4100.0 nM 5.39
CHEMBL346361 IC50 = 4500.0 nM 5.35
CHEMBL155406 IC50 = 7000.0 nM 5.16
CHEMBL157722 IC50 = 13000.0 nM 4.89
CHEMBL156415 IC50 = 17000.0 nM 4.77
CHEMBL422701 IC50 = 39000.0 nM 4.41
CHEMBL156814 IC50 = 44000.0 nM 4.36
CHEMBL158078 IC50 = 100000.0 nM 4.00
CHEMBL316561 PROGLUMIDE IC50 = 900000.0 nM -