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Assay Detail

CHEMBL616433

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

Binding
Affinity for 5-hydroxytryptamine 1B receptor subtype
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1B (CHEMBL1898)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Arylpiperazide derivatives of phenylpiperazines as a new class of potent and selective 5-HT1B receptor antagonists
Jorand-Lebrun C, Pauwels P, Palmier C, Chopin P, Moret C, Marien M, Halazy S
Bioorg Med Chem Lett (1997) 7 : 3183 -3188
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.38 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15928 GR-127935 1 9.85
CHEMBL325359 1 9.30
CHEMBL321818 1 9.10
CHEMBL111302 1 8.89
CHEMBL323986 1 8.74
CHEMBL430500 1 8.70
CHEMBL105970 1 8.64
CHEMBL108722 1 8.10
CHEMBL108645 1 8.08
CHEMBL281350 SB-224289 1 8.00
CHEMBL106807 1 7.96
CHEMBL325131 1 7.75
CHEMBL110601 1 7.40
CHEMBL107772 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15928 GR-127935 Ki = 0.14 nM 9.85
CHEMBL325359 Ki = 0.5 nM 9.30
CHEMBL321818 Ki = 0.8 nM 9.10
CHEMBL111302 Ki = 1.3 nM 8.89
CHEMBL323986 Ki = 1.8 nM 8.74
CHEMBL430500 Ki = 2.0 nM 8.70
CHEMBL105970 Ki = 2.3 nM 8.64
CHEMBL108722 Ki = 8.0 nM 8.10
CHEMBL108645 Ki = 8.4 nM 8.08
CHEMBL281350 SB-224289 Ki = 10.0 nM 8.00
CHEMBL106807 Ki = 11.0 nM 7.96
CHEMBL325131 Ki = 18.0 nM 7.75
CHEMBL110601 Ki = 40.0 nM 7.40
CHEMBL107772 Ki = 150.0 nM 6.82