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Assay Detail

CHEMBL674063

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

Binding
Binding affinity for [3H]raclopride-labeled dopamine receptor D2 in rat striatum
17
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
Lin CH, Haadsma-Svensson SR, Phillips G, Lahti RA, McCall RB, Piercey MF, Schreur PJ, Von Voigtlander PF, Smith MW, Chidester CG.
J Med Chem (1993) 36 : 1069 -1083
PubMed 8097538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.16 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11066 2 8.70
CHEMBL11363 2 8.52
CHEMBL275689 2 7.96
CHEMBL267557 1 7.33
CHEMBL11771 1 6.93
CHEMBL11294 1 6.37
CHEMBL275057 1 6.33
CHEMBL273601 1 6.13
CHEMBL11388 1 6.06
CHEMBL11065 1 -
CHEMBL11170 1 -
CHEMBL275008 1 -
CHEMBL56 8-OH-DPAT 1 -
CHEMBL11880 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11066 Ki = 2.0 nM 8.70
CHEMBL11363 Ki = 3.0 nM 8.52
CHEMBL275689 Ki = 11.0 nM 7.96
CHEMBL11066 Ki = 17.0 nM 7.77
CHEMBL11363 Ki = 47.0 nM 7.33
CHEMBL267557 Ki = 47.0 nM 7.33
CHEMBL11771 Ki = 118.0 nM 6.93
CHEMBL275689 Ki = 296.0 nM 6.53
CHEMBL11294 Ki = 429.0 nM 6.37
CHEMBL275057 Ki = 465.0 nM 6.33
CHEMBL273601 Ki = 748.0 nM 6.13
CHEMBL11388 Ki = 877.0 nM 6.06
CHEMBL11880 Ki > 10000.0 nM -
CHEMBL56 8-OH-DPAT Ki > 1000.0 nM -
CHEMBL275008 Ki > 1000.0 nM -
CHEMBL11170 Ki > 1000.0 nM -
CHEMBL11065 Ki > 630.0 nM -