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Assay Detail

CHEMBL616642

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

Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL ↗
45
Total Activities
44
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-(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
IC50 45 7.36 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL159396 — — 1 9.30
CHEMBL296161 — — 1 8.89
CHEMBL161176 — — 1 8.62
CHEMBL162930 — — 1 8.13
CHEMBL163386 — — 1 8.02
CHEMBL65367 — — 1 7.96
CHEMBL128 SUMATRIPTAN 4.0 1 7.96
CHEMBL162463 — — 1 7.89
CHEMBL163462 — — 2 7.89
CHEMBL351346 — — 1 7.89
CHEMBL331612 — — 1 7.82
CHEMBL348962 — — 1 7.77
CHEMBL163573 — — 1 7.75
CHEMBL162805 — — 1 7.75
CHEMBL352159 — — 1 7.75
CHEMBL161723 — — 1 7.70
CHEMBL422366 — — 1 7.66
CHEMBL162858 — — 1 7.64
CHEMBL164111 — — 1 7.57
CHEMBL116092 — — 1 7.55
CHEMBL164413 — — 1 7.44
CHEMBL420965 — — 1 7.43
CHEMBL162722 — — 1 7.35
CHEMBL163114 — — 1 7.34
CHEMBL163127 — — 1 7.25
CHEMBL161696 — — 1 7.23
CHEMBL292779 — — 1 7.14
CHEMBL161970 — — 1 7.11
CHEMBL119668 — — 1 7.08
CHEMBL352123 — — 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL159396 — IC50 = 0.5 nM 9.30
CHEMBL296161 — IC50 = 1.3 nM 8.89
CHEMBL161176 — IC50 = 2.4 nM 8.62
CHEMBL162930 — IC50 = 7.4 nM 8.13
CHEMBL163386 — IC50 = 9.5 nM 8.02
CHEMBL65367 — IC50 = 11.0 nM 7.96
CHEMBL128 SUMATRIPTAN IC50 = 11.0 nM 7.96
CHEMBL162463 — IC50 = 13.0 nM 7.89
CHEMBL163462 — IC50 = 13.0 nM 7.89
CHEMBL351346 — IC50 = 13.0 nM 7.89
CHEMBL331612 — IC50 = 15.0 nM 7.82
CHEMBL348962 — IC50 = 17.0 nM 7.77
CHEMBL163573 — IC50 = 18.0 nM 7.75
CHEMBL352159 — IC50 = 18.0 nM 7.75
CHEMBL162805 — IC50 = 18.0 nM 7.75
CHEMBL161723 — IC50 = 20.0 nM 7.70
CHEMBL422366 — IC50 = 22.0 nM 7.66
CHEMBL162858 — IC50 = 23.0 nM 7.64
CHEMBL164111 — IC50 = 27.0 nM 7.57
CHEMBL116092 — IC50 = 28.0 nM 7.55
CHEMBL164413 — IC50 = 36.0 nM 7.44
CHEMBL420965 — IC50 = 37.0 nM 7.43
CHEMBL162722 — IC50 = 45.0 nM 7.35
CHEMBL163114 — IC50 = 46.0 nM 7.34
CHEMBL163462 — IC50 = 55.0 nM 7.26
CHEMBL163127 — IC50 = 56.0 nM 7.25
CHEMBL161696 — IC50 = 59.0 nM 7.23
CHEMBL292779 — IC50 = 72.0 nM 7.14
CHEMBL161970 — IC50 = 78.0 nM 7.11
CHEMBL119668 — IC50 = 83.0 nM 7.08
CHEMBL352123 — IC50 = 85.0 nM 7.07
CHEMBL351311 — IC50 = 93.0 nM 7.03
CHEMBL116031 — IC50 = 98.0 nM 7.01
CHEMBL164035 — IC50 = 102.0 nM 6.99
CHEMBL115750 — IC50 = 120.0 nM 6.92
CHEMBL347665 — IC50 = 130.0 nM 6.89
CHEMBL274001 — IC50 = 145.0 nM 6.84
CHEMBL117633 — IC50 = 166.0 nM 6.78
CHEMBL119785 — IC50 = 260.0 nM 6.58
CHEMBL162899 — IC50 = 282.0 nM 6.55
CHEMBL163376 — IC50 = 282.0 nM 6.55
CHEMBL324931 — IC50 = 304.0 nM 6.52
CHEMBL117249 — IC50 = 309.0 nM 6.51
CHEMBL161969 — IC50 = 3900.0 nM 5.41
CHEMBL422191 — IC50 = 5100.0 nM 5.29