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Assay Detail

CHEMBL616668

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

Functional
Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1D (CHEMBL1983)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.
Sternfeld F, Guiblin AR, Jelley RA, Matassa VG, Reeve AJ, Hunt PA, Beer MS, Heald A, Stanton JA, Sohal B, Watt AP, Street LJ.
J Med Chem (1999) 42 : 677 -690
PubMed 10052975 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 29 8.51 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL164046 1 9.52
CHEMBL296161 1 9.40
CHEMBL160070 1 9.30
CHEMBL159759 1 9.20
CHEMBL420965 1 9.10
CHEMBL349185 1 8.89
CHEMBL117579 1 8.82
CHEMBL159483 1 8.77
CHEMBL351303 1 8.74
CHEMBL161410 1 8.68
CHEMBL326371 1 8.68
CHEMBL116092 1 8.64
CHEMBL349041 1 8.55
CHEMBL424154 1 8.52
CHEMBL159683 1 8.52
CHEMBL350153 1 8.49
CHEMBL161780 1 8.46
CHEMBL159819 1 8.39
CHEMBL348864 1 8.35
CHEMBL161192 1 8.31
CHEMBL348815 1 8.21
CHEMBL349528 1 8.11
CHEMBL441296 1 8.06
CHEMBL161066 1 8.02
CHEMBL349390 1 8.00
CHEMBL159733 1 7.96
CHEMBL128 SUMATRIPTAN 4.0 1 7.85
CHEMBL420874 1 7.82
CHEMBL435060 1 7.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL164046 EC50 = 0.3 nM 9.52
CHEMBL296161 EC50 = 0.4 nM 9.40
CHEMBL160070 EC50 = 0.5 nM 9.30
CHEMBL159759 EC50 = 0.63 nM 9.20
CHEMBL420965 EC50 = 0.8 nM 9.10
CHEMBL349185 EC50 = 1.3 nM 8.89
CHEMBL117579 EC50 = 1.5 nM 8.82
CHEMBL159483 EC50 = 1.7 nM 8.77
CHEMBL351303 EC50 = 1.8 nM 8.74
CHEMBL161410 EC50 = 2.1 nM 8.68
CHEMBL326371 EC50 = 2.1 nM 8.68
CHEMBL116092 EC50 = 2.3 nM 8.64
CHEMBL349041 EC50 = 2.8 nM 8.55
CHEMBL424154 EC50 = 3.0 nM 8.52
CHEMBL159683 EC50 = 3.0 nM 8.52
CHEMBL350153 EC50 = 3.2 nM 8.49
CHEMBL161780 EC50 = 3.5 nM 8.46
CHEMBL159819 EC50 = 4.1 nM 8.39
CHEMBL348864 EC50 = 4.5 nM 8.35
CHEMBL161192 EC50 = 4.9 nM 8.31
CHEMBL348815 EC50 = 6.2 nM 8.21
CHEMBL349528 EC50 = 7.8 nM 8.11
CHEMBL441296 EC50 = 8.7 nM 8.06
CHEMBL161066 EC50 = 9.5 nM 8.02
CHEMBL349390 EC50 = 10.0 nM 8.00
CHEMBL159733 EC50 = 11.0 nM 7.96
CHEMBL128 SUMATRIPTAN EC50 = 14.0 nM 7.85
CHEMBL420874 EC50 = 15.0 nM 7.82
CHEMBL435060 EC50 = 31.0 nM 7.51