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Assay Detail

CHEMBL674062

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

Binding
Binding affinity against [3H]raclopride-labeled dopamine receptor D2 in rat striatum.
20
Total Activities
20
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. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.
Lin CH, Haadsma-Svensson SR, Lahti RA, McCall RB, Piercey MF, Schreur PJ, Von Voigtlander PF, Smith MW, Chidester CG.
J Med Chem (1993) 36 : 1053 -1068
PubMed 8097537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.26 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10270 1 8.28
CHEMBL286205 1 7.89
CHEMBL280955 1 7.60
CHEMBL24588 1 7.48
CHEMBL10570 1 7.38
CHEMBL10408 1 7.31
CHEMBL25483 1 7.27
CHEMBL280137 1 7.20
CHEMBL284585 1 7.17
CHEMBL24222 1 7.00
CHEMBL285873 1 6.70
CHEMBL275543 1 6.59
CHEMBL418705 1 6.57
CHEMBL26560 1 -
CHEMBL568290 1 -
CHEMBL25177 1 -
CHEMBL56 8-OH-DPAT 1 -
CHEMBL10677 1 -
CHEMBL25691 1 -
CHEMBL24532 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10270 Ki = 5.3 nM 8.28
CHEMBL286205 Ki = 13.0 nM 7.89
CHEMBL280955 Ki = 25.0 nM 7.60
CHEMBL24588 Ki = 33.0 nM 7.48
CHEMBL10570 Ki = 42.0 nM 7.38
CHEMBL10408 Ki = 49.0 nM 7.31
CHEMBL25483 Ki = 54.0 nM 7.27
CHEMBL280137 Ki = 63.0 nM 7.20
CHEMBL284585 Ki = 67.0 nM 7.17
CHEMBL24222 Ki = 99.0 nM 7.00
CHEMBL285873 Ki = 198.0 nM 6.70
CHEMBL275543 Ki = 259.0 nM 6.59
CHEMBL418705 Ki = 270.0 nM 6.57
CHEMBL26560 Ki > 1000.0 nM -
CHEMBL568290 Ki > 1000.0 nM -
CHEMBL25177 Ki > 1000.0 nM -
CHEMBL56 8-OH-DPAT Ki > 1000.0 nM -
CHEMBL10677 Ki > 1000.0 nM -
CHEMBL25691 Ki > 10000.0 nM -
CHEMBL24532 Ki > 10000.0 nM -