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Assay Detail

CHEMBL651986

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

Binding
Binding affinity against rat Alpha-1 adrenergic receptor.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
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 18 6.67 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9921 1 7.50
CHEMBL273923 1 7.16
CHEMBL9669 1 7.08
CHEMBL9467 1 7.02
CHEMBL9746 1 6.97
CHEMBL9870 1 6.93
CHEMBL9452 1 6.86
CHEMBL276156 1 6.78
CHEMBL275943 1 6.67
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 6.63
CHEMBL274866 1 6.47
CHEMBL9429 1 6.43
CHEMBL266250 1 6.29
CHEMBL9666 1 6.29
CHEMBL269784 1 6.17
CHEMBL9434 PHENYLPIPERAZINE 1 6.10
CHEMBL269521 MK-212 1 6.04
CHEMBL267153 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9921 Ki = 31.8 nM 7.50
CHEMBL273923 Ki = 70.0 nM 7.16
CHEMBL9669 Ki = 84.0 nM 7.08
CHEMBL9467 Ki = 96.0 nM 7.02
CHEMBL9746 Ki = 108.0 nM 6.97
CHEMBL9870 Ki = 117.0 nM 6.93
CHEMBL9452 Ki = 139.0 nM 6.86
CHEMBL276156 Ki = 168.0 nM 6.78
CHEMBL275943 Ki = 214.0 nM 6.67
CHEMBL478 CHLOROPHENYLPIPERAZINE Ki = 236.0 nM 6.63
CHEMBL274866 Ki = 337.0 nM 6.47
CHEMBL9429 Ki = 373.0 nM 6.43
CHEMBL266250 Ki = 516.0 nM 6.29
CHEMBL9666 Ki = 510.0 nM 6.29
CHEMBL269784 Ki = 670.0 nM 6.17
CHEMBL9434 PHENYLPIPERAZINE Ki = 794.0 nM 6.10
CHEMBL269521 MK-212 Ki = 913.0 nM 6.04
CHEMBL267153 Ki > 1000.0 nM -