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Assay Detail

CHEMBL679997

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

Binding
Binding affinity against [125 I][4Tyr]-bombesin labeled cloned human GRP(gastrin releasing peptide) receptors stably expressed in CHO cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Gastrin-releasing peptide receptor (CHEMBL4959)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

PD 165929 the first high affinity non-peptide neuromedin-B (NMB) receptor selective antagonist
Eden J, Hall M, Higginbottom M, Horwell D, Howson W, Hughes J, Jordan R, Lewthwaite R, Martin K, McKnight A, O'Toole J, Pinnock R, Pritchard M, Suman-Chauhan N, Williams S
Bioorg Med Chem Lett (1996) 6 : 2617 -2622
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 8.26 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437027 BOMBESIN 1.0 1 9.82
CHEMBL269432 1 9.15
CHEMBL328591 1 5.82
CHEMBL329561 1 -
CHEMBL87090 1 -
CHEMBL89153 1 -
CHEMBL315859 1 -
CHEMBL315660 1 -
CHEMBL312851 1 -
CHEMBL328230 1 -
CHEMBL1907682 1 -
CHEMBL89795 1 -
CHEMBL313114 1 -
CHEMBL88174 1 -
CHEMBL89075 1 -
CHEMBL406037 1 -
CHEMBL313829 1 -
CHEMBL1907865 1 -
CHEMBL86828 1 -
CHEMBL92274 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437027 BOMBESIN Ki = 0.15 nM 9.82
CHEMBL269432 Ki = 0.7 nM 9.15
CHEMBL328591 Ki = 1500.0 nM 5.82
CHEMBL329561 Ki > 10000.0 nM -
CHEMBL87090 Ki > 10000.0 nM -
CHEMBL89153 Ki > 10000.0 nM -
CHEMBL315859 Ki > 10000.0 nM -
CHEMBL315660 Ki > 10000.0 nM -
CHEMBL312851 Ki > 10000.0 nM -
CHEMBL328230 Ki > 10000.0 nM -
CHEMBL1907682 Ki > 10000.0 nM -
CHEMBL89795 Ki > 10000.0 nM -
CHEMBL313114 Ki > 10000.0 nM -
CHEMBL88174 Ki > 10000.0 nM -
CHEMBL89075 Ki > 10000.0 nM -
CHEMBL406037 Ki > 10000.0 nM -
CHEMBL313829 Ki > 10000.0 nM -
CHEMBL1907865 Ki > 10000.0 nM -
CHEMBL86828 Ki > 10000.0 nM -
CHEMBL92274 Ki > 10000.0 nM -