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Assay Detail

CHEMBL617040

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 human 5-hydroxytryptamine 1D receptor.
28
Total Activities
28
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-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
Chambers MS, Street LJ, Goodacre S, Hobbs SC, Hunt P, Jelley RA, Matassa VG, Reeve AJ, Sternfeld F, Beer MS, Stanton JA, Rathbone D, Watt AP, MacLeod AM.
J Med Chem (1999) 42 : 691 -705
PubMed 10052976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 9.04 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL161176 1 9.70
CHEMBL163462 1 9.70
CHEMBL65367 1 9.70
CHEMBL162722 1 9.52
CHEMBL163386 1 9.52
CHEMBL163573 1 9.52
CHEMBL164111 1 9.52
CHEMBL161723 1 9.52
CHEMBL422366 1 9.52
CHEMBL162805 1 9.30
CHEMBL159396 1 9.22
CHEMBL119668 1 9.15
CHEMBL164035 1 9.10
CHEMBL162858 1 9.00
CHEMBL292779 1 9.00
CHEMBL347665 1 8.96
CHEMBL161696 1 8.92
CHEMBL116031 1 8.85
CHEMBL115750 1 8.82
CHEMBL348962 1 8.77
CHEMBL117633 1 8.77
CHEMBL119785 1 8.74
CHEMBL164413 1 8.70
CHEMBL352159 1 8.64
CHEMBL352123 1 8.40
CHEMBL163127 1 8.21
CHEMBL162899 1 8.12
CHEMBL351311 1 8.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL161176 EC50 = 0.2 nM 9.70
CHEMBL163462 EC50 = 0.2 nM 9.70
CHEMBL65367 EC50 = 0.2 nM 9.70
CHEMBL162722 EC50 = 0.3 nM 9.52
CHEMBL163386 EC50 = 0.3 nM 9.52
CHEMBL163573 EC50 = 0.3 nM 9.52
CHEMBL164111 EC50 = 0.3 nM 9.52
CHEMBL161723 EC50 = 0.3 nM 9.52
CHEMBL422366 EC50 = 0.3 nM 9.52
CHEMBL162805 EC50 = 0.5 nM 9.30
CHEMBL159396 EC50 = 0.6 nM 9.22
CHEMBL119668 EC50 = 0.7 nM 9.15
CHEMBL164035 EC50 = 0.8 nM 9.10
CHEMBL162858 EC50 = 1.0 nM 9.00
CHEMBL292779 EC50 = 1.0 nM 9.00
CHEMBL347665 EC50 = 1.1 nM 8.96
CHEMBL161696 EC50 = 1.2 nM 8.92
CHEMBL116031 EC50 = 1.4 nM 8.85
CHEMBL115750 EC50 = 1.5 nM 8.82
CHEMBL348962 EC50 = 1.7 nM 8.77
CHEMBL117633 EC50 = 1.7 nM 8.77
CHEMBL119785 EC50 = 1.8 nM 8.74
CHEMBL164413 EC50 = 2.0 nM 8.70
CHEMBL352159 EC50 = 2.3 nM 8.64
CHEMBL352123 EC50 = 4.0 nM 8.40
CHEMBL163127 EC50 = 6.1 nM 8.21
CHEMBL162899 EC50 = 7.5 nM 8.12
CHEMBL351311 EC50 = 7.8 nM 8.11