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Assay Detail

CHEMBL672342

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

Binding
Affinity for Dopamine receptor D2
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
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 14 7.88 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.70
CHEMBL85 RISPERIDONE 4.0 1 8.68
CHEMBL171903 1 8.52
CHEMBL176356 1 8.17
CHEMBL173315 1 8.04
CHEMBL178797 1 7.51
CHEMBL176990 1 7.47
CHEMBL174949 1 7.17
CHEMBL176476 1 7.08
CHEMBL366504 1 6.43
CHEMBL367981 1 -
CHEMBL176363 1 -
CHEMBL366377 1 -
CHEMBL160430 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.2 nM 9.70
CHEMBL85 RISPERIDONE Ki = 2.1 nM 8.68
CHEMBL171903 Ki = 3.0 nM 8.52
CHEMBL176356 Ki = 6.8 nM 8.17
CHEMBL173315 Ki = 9.2 nM 8.04
CHEMBL178797 Ki = 31.0 nM 7.51
CHEMBL176990 Ki = 34.0 nM 7.47
CHEMBL174949 Ki = 67.0 nM 7.17
CHEMBL176476 Ki = 83.0 nM 7.08
CHEMBL366504 Ki = 370.0 nM 6.43
CHEMBL367981 Ki > 1000.0 nM -
CHEMBL176363 Ki > 1000.0 nM -
CHEMBL366377 Ki > 1000.0 nM -
CHEMBL160430 Ki > 1000.0 nM -