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Assay Detail

CHEMBL617304

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

Binding
Binding affinity to recombinant human 5-hydroxytryptamine 1D receptor alpha
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors.
Perez M, Fourrier C, Sigogneau I, Pauwels PJ, Palmier C, John GW, Valentin JP, Halazy S.
J Med Chem (1995) 38 : 3602 -3607
PubMed 7658447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 8.86 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1203216 1 9.59
CHEMBL121207 1 9.47
CHEMBL120514 1 9.42
CHEMBL334323 1 9.38
CHEMBL121901 1 9.25
CHEMBL332142 1 9.24
CHEMBL119927 1 9.04
CHEMBL1185 ZOLMITRIPTAN 4.0 1 9.04
CHEMBL121499 1 9.03
CHEMBL117157 1 9.00
CHEMBL421064 1 8.92
CHEMBL120272 1 8.92
CHEMBL331037 1 8.89
CHEMBL116314 1 8.85
CHEMBL331240 1 8.85
CHEMBL334193 1 8.77
CHEMBL120480 1 8.74
CHEMBL120055 1 8.68
CHEMBL324289 1 8.60
CHEMBL334159 1 8.54
CHEMBL39 SEROTONIN 3.0 1 8.32
CHEMBL332063 1 8.16
CHEMBL128 SUMATRIPTAN 4.0 1 8.07
CHEMBL905 RIZATRIPTAN 4.0 1 7.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1203216 Ki = 0.26 nM 9.59
CHEMBL121207 Ki = 0.34 nM 9.47
CHEMBL120514 Ki = 0.38 nM 9.42
CHEMBL334323 Ki = 0.42 nM 9.38
CHEMBL121901 Ki = 0.56 nM 9.25
CHEMBL332142 Ki = 0.58 nM 9.24
CHEMBL119927 Ki = 0.92 nM 9.04
CHEMBL1185 ZOLMITRIPTAN Ki = 0.92 nM 9.04
CHEMBL121499 Ki = 0.93 nM 9.03
CHEMBL117157 Ki = 1.0 nM 9.00
CHEMBL421064 Ki = 1.2 nM 8.92
CHEMBL120272 Ki = 1.2 nM 8.92
CHEMBL331037 Ki = 1.3 nM 8.89
CHEMBL116314 Ki = 1.4 nM 8.85
CHEMBL331240 Ki = 1.4 nM 8.85
CHEMBL334193 Ki = 1.7 nM 8.77
CHEMBL120480 Ki = 1.8 nM 8.74
CHEMBL120055 Ki = 2.08 nM 8.68
CHEMBL324289 Ki = 2.5 nM 8.60
CHEMBL334159 Ki = 2.92 nM 8.54
CHEMBL39 SEROTONIN Ki = 4.8 nM 8.32
CHEMBL332063 Ki = 6.9 nM 8.16
CHEMBL128 SUMATRIPTAN Ki = 8.5 nM 8.07
CHEMBL905 RIZATRIPTAN Ki = 13.5 nM 7.87