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Assay Detail

CHEMBL617042

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

Functional
Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor.
16
Total Activities
15
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

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
EC50 16 8.53 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296161 1 9.35
CHEMBL333341 1 9.05
CHEMBL420965 1 9.03
CHEMBL313714 1 8.96
CHEMBL331970 1 8.82
CHEMBL117579 1 8.80
CHEMBL304857 1 8.80
CHEMBL118012 1 8.74
CHEMBL326371 1 8.68
CHEMBL116092 1 8.59
CHEMBL159819 1 8.39
CHEMBL117046 1 8.10
CHEMBL905 RIZATRIPTAN 4.0 1 8.08
CHEMBL420874 2 7.82
CHEMBL128 SUMATRIPTAN 4.0 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296161 EC50 = 0.45 nM 9.35
CHEMBL333341 EC50 = 0.9 nM 9.05
CHEMBL420965 EC50 = 0.93 nM 9.03
CHEMBL313714 EC50 = 1.1 nM 8.96
CHEMBL331970 EC50 = 1.5 nM 8.82
CHEMBL117579 EC50 = 1.6 nM 8.80
CHEMBL304857 EC50 = 1.6 nM 8.80
CHEMBL118012 EC50 = 1.8 nM 8.74
CHEMBL326371 EC50 = 2.1 nM 8.68
CHEMBL116092 EC50 = 2.6 nM 8.59
CHEMBL159819 EC50 = 4.1 nM 8.39
CHEMBL117046 EC50 = 8.0 nM 8.10
CHEMBL905 RIZATRIPTAN EC50 = 8.4 nM 8.08
CHEMBL420874 EC50 = 15.0 nM 7.82
CHEMBL128 SUMATRIPTAN EC50 = 16.0 nM 7.80
CHEMBL420874 EC50 = 33.0 nM 7.48