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Assay Detail

CHEMBL616139

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

Binding
Binding affinity for cloned human 5-hydroxytryptamine 1A receptor
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
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 23 7.44 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL120480 1 8.29
CHEMBL332142 1 8.28
CHEMBL120055 1 8.10
CHEMBL331037 1 7.99
CHEMBL421064 1 7.98
CHEMBL121207 1 7.89
CHEMBL332063 1 7.87
CHEMBL120272 1 7.82
CHEMBL119927 1 7.82
CHEMBL324289 1 7.80
CHEMBL334323 1 7.62
CHEMBL1203216 1 7.39
CHEMBL120514 1 7.37
CHEMBL116314 1 7.29
CHEMBL334193 1 7.21
CHEMBL121901 1 7.16
CHEMBL331240 1 7.11
CHEMBL1185 ZOLMITRIPTAN 4.0 1 7.11
CHEMBL117157 1 7.02
CHEMBL121499 1 6.89
CHEMBL905 RIZATRIPTAN 4.0 1 6.53
CHEMBL128 SUMATRIPTAN 4.0 1 6.36
CHEMBL334159 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL120480 Ki = 5.1 nM 8.29
CHEMBL332142 Ki = 5.2 nM 8.28
CHEMBL120055 Ki = 8.0 nM 8.10
CHEMBL331037 Ki = 10.2 nM 7.99
CHEMBL421064 Ki = 10.4 nM 7.98
CHEMBL121207 Ki = 12.8 nM 7.89
CHEMBL332063 Ki = 13.6 nM 7.87
CHEMBL120272 Ki = 15.1 nM 7.82
CHEMBL119927 Ki = 15.0 nM 7.82
CHEMBL324289 Ki = 15.9 nM 7.80
CHEMBL334323 Ki = 24.0 nM 7.62
CHEMBL1203216 Ki = 40.3 nM 7.39
CHEMBL120514 Ki = 42.6 nM 7.37
CHEMBL116314 Ki = 50.7 nM 7.29
CHEMBL334193 Ki = 61.0 nM 7.21
CHEMBL121901 Ki = 68.9 nM 7.16
CHEMBL331240 Ki = 77.8 nM 7.11
CHEMBL1185 ZOLMITRIPTAN Ki = 78.6 nM 7.11
CHEMBL117157 Ki = 95.0 nM 7.02
CHEMBL121499 Ki = 130.0 nM 6.89
CHEMBL905 RIZATRIPTAN Ki = 293.0 nM 6.53
CHEMBL128 SUMATRIPTAN Ki = 440.0 nM 6.36
CHEMBL334159 Ki = 607.0 nM 6.22