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Assay Detail

CHEMBL645395

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

Binding
Affinity for alpha-1 adrenergic receptor
12
Total Activities
12
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

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.
Maryanoff BE, McComsey DF, Martin GE, Shank RP.
Bioorg Med Chem Lett (1998) 8 : 983 -988
PubMed 9871525 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.53 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 8.52
CHEMBL176990 1 7.85
CHEMBL178797 1 7.68
CHEMBL176356 1 7.66
CHEMBL54 HALOPERIDOL 4.0 1 7.64
CHEMBL171903 1 7.46
CHEMBL174949 1 7.24
CHEMBL367981 1 6.18
CHEMBL176363 1 -
CHEMBL366377 1 -
CHEMBL160430 1 -
CHEMBL366504 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 3.0 nM 8.52
CHEMBL176990 Ki = 14.0 nM 7.85
CHEMBL178797 Ki = 21.0 nM 7.68
CHEMBL176356 Ki = 22.0 nM 7.66
CHEMBL54 HALOPERIDOL Ki = 23.0 nM 7.64
CHEMBL171903 Ki = 35.0 nM 7.46
CHEMBL174949 Ki = 57.0 nM 7.24
CHEMBL367981 Ki = 660.0 nM 6.18
CHEMBL176363 Ki > 500.0 nM -
CHEMBL366377 Ki < 1000.0 nM -
CHEMBL160430 Ki < 1000.0 nM -
CHEMBL366504 Ki > 100.0 nM -