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Assay Detail

CHEMBL616534

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

Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptor
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

(R)-3-(N-methylpyrrolidin-2-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity h5-HT1B/1D ligands.
Egle I, MacLean N, Demchyshyn L, Edwards L, Slassi A, Tehim A.
Bioorg Med Chem Lett (2003) 13 : 3419 -3421
PubMed 14505640 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 8.09 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113950 1 8.82
CHEMBL115663 1 8.82
CHEMBL113994 1 8.62
CHEMBL114571 1 8.52
CHEMBL117397 1 8.49
CHEMBL113893 1 8.42
CHEMBL114780 1 8.42
CHEMBL431866 1 8.38
CHEMBL325175 1 8.32
CHEMBL334259 1 8.24
CHEMBL128 SUMATRIPTAN 4.0 1 8.11
CHEMBL332484 1 7.96
CHEMBL113868 1 7.89
CHEMBL115941 1 7.85
CHEMBL323603 1 7.85
CHEMBL116876 1 7.77
CHEMBL323666 1 7.64
CHEMBL323705 1 7.41
CHEMBL115415 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113950 Ki = 1.5 nM 8.82
CHEMBL115663 Ki = 1.5 nM 8.82
CHEMBL113994 Ki = 2.4 nM 8.62
CHEMBL114571 Ki = 3.0 nM 8.52
CHEMBL117397 Ki = 3.2 nM 8.49
CHEMBL113893 Ki = 3.8 nM 8.42
CHEMBL114780 Ki = 3.8 nM 8.42
CHEMBL431866 Ki = 4.2 nM 8.38
CHEMBL325175 Ki = 4.8 nM 8.32
CHEMBL334259 Ki = 5.8 nM 8.24
CHEMBL128 SUMATRIPTAN Ki = 7.7 nM 8.11
CHEMBL332484 Ki = 11.0 nM 7.96
CHEMBL113868 Ki = 13.0 nM 7.89
CHEMBL115941 Ki = 14.0 nM 7.85
CHEMBL323603 Ki = 14.0 nM 7.85
CHEMBL116876 Ki = 17.0 nM 7.77
CHEMBL323666 Ki = 23.0 nM 7.64
CHEMBL323705 Ki = 39.0 nM 7.41
CHEMBL115415 Ki = 610.0 nM 6.21