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Assay Detail

CHEMBL616637

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

Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
20
Total Activities
19
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

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

Publication

3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.
Castro JL, Street LJ, Guiblin AR, Jelley RA, Russell MG, Sternfeld F, Beer MS, Stanton JA, Matassa VG.
J Med Chem (1997) 40 : 3497 -3500
PubMed 9357514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.12 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296161 1 8.85
CHEMBL331612 1 7.82
CHEMBL128 SUMATRIPTAN 4.0 1 7.80
CHEMBL333341 1 7.55
CHEMBL116092 1 7.52
CHEMBL117579 1 7.48
CHEMBL331970 1 7.46
CHEMBL905 RIZATRIPTAN 4.0 1 7.39
CHEMBL420965 1 7.33
CHEMBL159819 1 7.30
CHEMBL326371 1 7.06
CHEMBL118012 1 6.94
CHEMBL117046 1 6.90
CHEMBL420874 2 6.84
CHEMBL304857 1 6.84
CHEMBL313714 1 6.73
CHEMBL324287 1 6.68
CHEMBL330803 1 6.25
CHEMBL51 KETANSERIN 3.0 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296161 IC50 = 1.4 nM 8.85
CHEMBL331612 IC50 = 15.0 nM 7.82
CHEMBL128 SUMATRIPTAN IC50 = 16.0 nM 7.80
CHEMBL333341 IC50 = 28.0 nM 7.55
CHEMBL116092 IC50 = 30.2 nM 7.52
CHEMBL117579 IC50 = 33.0 nM 7.48
CHEMBL331970 IC50 = 35.0 nM 7.46
CHEMBL905 RIZATRIPTAN IC50 = 41.0 nM 7.39
CHEMBL420965 IC50 = 47.0 nM 7.33
CHEMBL159819 IC50 = 50.0 nM 7.30
CHEMBL326371 IC50 = 88.0 nM 7.06
CHEMBL118012 IC50 = 114.0 nM 6.94
CHEMBL117046 IC50 = 125.0 nM 6.90
CHEMBL420874 IC50 = 146.0 nM 6.84
CHEMBL304857 IC50 = 145.0 nM 6.84
CHEMBL313714 IC50 = 185.0 nM 6.73
CHEMBL324287 IC50 = 210.0 nM 6.68
CHEMBL420874 IC50 = 280.0 nM 6.55
CHEMBL330803 IC50 = 568.0 nM 6.25
CHEMBL51 KETANSERIN IC50 = 6500.0 nM 5.19