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Assay Detail

CHEMBL615486

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

Binding
Inhibition of [3H]5-HT radioligand binding against 5-hydroxytryptamine 1 receptor
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Serotonin 1 (5-HT1) receptor (CHEMBL2095159)
Type PROTEIN FAMILY
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 10 7.33 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9669 1 7.72
CHEMBL9452 1 7.71
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 7.60
CHEMBL275943 1 7.58
CHEMBL9666 1 7.54
CHEMBL273923 1 7.37
CHEMBL9429 1 7.24
CHEMBL269784 1 7.06
CHEMBL9434 PHENYLPIPERAZINE 1 6.83
CHEMBL267153 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9669 Ki = 19.0 nM 7.72
CHEMBL9452 Ki = 19.3 nM 7.71
CHEMBL478 CHLOROPHENYLPIPERAZINE Ki = 25.0 nM 7.60
CHEMBL275943 Ki = 26.1 nM 7.58
CHEMBL9666 Ki = 29.0 nM 7.54
CHEMBL273923 Ki = 42.6 nM 7.37
CHEMBL9429 Ki = 57.9 nM 7.24
CHEMBL269784 Ki = 86.5 nM 7.06
CHEMBL9434 PHENYLPIPERAZINE Ki = 149.0 nM 6.83
CHEMBL267153 Ki = 250.0 nM 6.60