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Assay Detail

CHEMBL872909

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

Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
17
Total Activities
17
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 1B (CHEMBL3459)
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 17 7.78 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL276156 1 8.40
CHEMBL9452 1 8.40
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 8.36
CHEMBL9669 1 8.16
CHEMBL9467 1 8.09
CHEMBL9921 1 8.08
CHEMBL9841 1 7.93
CHEMBL273923 1 7.86
CHEMBL9870 1 7.80
CHEMBL9666 1 7.76
CHEMBL275943 1 7.66
CHEMBL9429 1 7.54
CHEMBL269784 1 7.51
CHEMBL267153 1 7.47
CHEMBL9746 1 7.35
CHEMBL9434 PHENYLPIPERAZINE 1 7.20
CHEMBL269521 MK-212 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL276156 Ki = 3.98 nM 8.40
CHEMBL9452 Ki = 4.0 nM 8.40
CHEMBL478 CHLOROPHENYLPIPERAZINE Ki = 4.4 nM 8.36
CHEMBL9669 Ki = 6.9 nM 8.16
CHEMBL9467 Ki = 8.2 nM 8.09
CHEMBL9921 Ki = 8.4 nM 8.08
CHEMBL9841 Ki = 11.7 nM 7.93
CHEMBL273923 Ki = 13.8 nM 7.86
CHEMBL9870 Ki = 15.9 nM 7.80
CHEMBL9666 Ki = 17.3 nM 7.76
CHEMBL275943 Ki = 21.8 nM 7.66
CHEMBL9429 Ki = 28.9 nM 7.54
CHEMBL269784 Ki = 30.8 nM 7.51
CHEMBL267153 Ki = 33.6 nM 7.47
CHEMBL9746 Ki = 44.6 nM 7.35
CHEMBL9434 PHENYLPIPERAZINE Ki = 63.3 nM 7.20
CHEMBL269521 MK-212 Ki = 178.0 nM 6.75