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Assay Detail

CHEMBL616953

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

Binding
Binding affinity at rat 5-hydroxytryptamine 1A receptor by [3H]WB-4101 displacement.
18
Total Activities
18
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 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy.
Martin GE, Elgin RJ, Mathiasen JR, Davis CB, Kesslick JM, Baldy WJ, Shank RP, DiStefano DL, Fedde CL, Scott MK.
J Med Chem (1989) 32 : 1052 -1056
PubMed 2565400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.58 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9669 1 8.12
CHEMBL273923 1 8.04
CHEMBL9666 1 8.02
CHEMBL9452 1 7.96
CHEMBL276156 1 7.90
CHEMBL9921 1 7.72
CHEMBL9870 1 7.71
CHEMBL9841 1 7.71
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 7.64
CHEMBL9467 1 7.64
CHEMBL275943 1 7.59
CHEMBL9746 1 7.56
CHEMBL266250 1 7.45
CHEMBL9429 1 7.37
CHEMBL269784 1 6.94
CHEMBL9434 PHENYLPIPERAZINE 1 6.83
CHEMBL269521 MK-212 1 6.70
CHEMBL267153 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9669 Ki = 7.6 nM 8.12
CHEMBL273923 Ki = 9.1 nM 8.04
CHEMBL9666 Ki = 9.5 nM 8.02
CHEMBL9452 Ki = 11.1 nM 7.96
CHEMBL276156 Ki = 12.5 nM 7.90
CHEMBL9921 Ki = 19.1 nM 7.72
CHEMBL9870 Ki = 19.4 nM 7.71
CHEMBL9841 Ki = 19.5 nM 7.71
CHEMBL478 CHLOROPHENYLPIPERAZINE Ki = 23.0 nM 7.64
CHEMBL9467 Ki = 22.7 nM 7.64
CHEMBL275943 Ki = 25.5 nM 7.59
CHEMBL9746 Ki = 27.4 nM 7.56
CHEMBL266250 Ki = 35.3 nM 7.45
CHEMBL9429 Ki = 43.0 nM 7.37
CHEMBL269784 Ki = 114.0 nM 6.94
CHEMBL9434 PHENYLPIPERAZINE Ki = 149.0 nM 6.83
CHEMBL269521 MK-212 Ki = 202.0 nM 6.70
CHEMBL267153 Ki ~ 322.0 nM -