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Assay Detail

CHEMBL652241

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

Binding
Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKB in mouse fore brain membranes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Gastrin/cholecystokinin type B receptor (CHEMBL2854)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Cholecystokinin analogues: The ergopeptine alkaloids as models of the active conformation of CCK
Kendrick DA, Ryder H, Semple G, Szelke M
Bioorg Med Chem Lett (1992) 2 : 9 -12
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.29 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278032 1 6.46
CHEMBL442 ERGOTAMINE 4.0 1 4.77
CHEMBL1732 DIHYDROERGOTAMINE 4.0 1 4.64
CHEMBL1403281 ERGOCRYPTINE 1 -
CHEMBL18727 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278032 IC50 = 350.0 nM 6.46
CHEMBL442 ERGOTAMINE IC50 = 17000.0 nM 4.77
CHEMBL1732 DIHYDROERGOTAMINE IC50 = 23000.0 nM 4.64
CHEMBL1403281 ERGOCRYPTINE IC50 > 80000.0 nM -
CHEMBL18727 IC50 > 80000.0 nM -