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Assay Detail

CHEMBL650353

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Binding
In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
Ashwood V, Brownhill V, Higginbottom M, Horwell DC, Hughes J, Lewthwaite RA, McKnight AT, Pinnock RD, Pritchard MC, Suman-Chauhan N, Webb C, Williams SC.
Bioorg Med Chem Lett (1998) 8 : 2589 -2594
PubMed 9873586 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.59 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413196 1 10.40
CHEMBL437027 BOMBESIN 1.0 1 9.82
CHEMBL314375 1 9.15
CHEMBL312926 1 8.43
CHEMBL85291 1 8.24
CHEMBL327388 1 8.19
CHEMBL433143 1 8.05
CHEMBL329650 1 7.77
CHEMBL87846 1 7.50
CHEMBL85400 1 7.48
CHEMBL313030 1 7.46
CHEMBL327840 1 7.43
CHEMBL403317 1 7.25
CHEMBL313346 1 7.07
CHEMBL327678 1 7.07
CHEMBL86370 1 7.05
CHEMBL90614 1 6.91
CHEMBL316085 1 6.83
CHEMBL88010 1 6.56
CHEMBL89734 1 6.39
CHEMBL87079 1 5.96
CHEMBL89813 1 5.90
CHEMBL86828 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413196 Ki = 0.04 nM 10.40
CHEMBL437027 BOMBESIN Ki = 0.15 nM 9.82
CHEMBL314375 Ki = 0.7 nM 9.15
CHEMBL312926 Ki = 3.7 nM 8.43
CHEMBL85291 Ki = 5.8 nM 8.24
CHEMBL327388 Ki = 6.4 nM 8.19
CHEMBL433143 Ki = 9.0 nM 8.05
CHEMBL329650 Ki = 17.0 nM 7.77
CHEMBL87846 Ki = 32.0 nM 7.50
CHEMBL85400 Ki = 33.0 nM 7.48
CHEMBL313030 Ki = 35.0 nM 7.46
CHEMBL327840 Ki = 37.0 nM 7.43
CHEMBL403317 Ki = 56.0 nM 7.25
CHEMBL313346 Ki = 85.0 nM 7.07
CHEMBL327678 Ki = 85.0 nM 7.07
CHEMBL86370 Ki = 89.0 nM 7.05
CHEMBL90614 Ki = 124.0 nM 6.91
CHEMBL316085 Ki = 149.0 nM 6.83
CHEMBL88010 Ki = 273.0 nM 6.56
CHEMBL89734 Ki = 404.0 nM 6.39
CHEMBL87079 Ki = 1096.0 nM 5.96
CHEMBL89813 Ki = 1254.0 nM 5.90
CHEMBL86828 Ki > 10000.0 nM -