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Assay Detail

CHEMBL671495

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

Binding
Binding affinity against Dopamine receptor D2 expressed in CHO-K1 cells, using [3H]U-86170 as the radioligand.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes.
Stjernlöf P, Ennis MD, Hansson LO, Hoffman RL, Ghazal NB, Sundell S, Smith MW, Svensson K, Carlsson A, Wikström H.
J Med Chem (1995) 38 : 2202 -2216
PubMed 7783152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.24 8.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL302172 1 8.13
CHEMBL303021 1 8.01
CHEMBL69562 1 7.85
CHEMBL65196 1 7.82
CHEMBL302171 1 7.77
CHEMBL308347 1 7.66
CHEMBL70589 1 7.62
CHEMBL306869 1 7.48
CHEMBL441256 1 7.19
CHEMBL71899 1 7.07
CHEMBL302373 1 6.79
CHEMBL302994 1 6.75
CHEMBL71395 1 6.69
CHEMBL303269 1 6.58
CHEMBL71804 1 6.38
CHEMBL71319 1 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL302172 Ki = 7.4 nM 8.13
CHEMBL303021 Ki = 9.8 nM 8.01
CHEMBL69562 Ki = 14.0 nM 7.85
CHEMBL65196 Ki = 15.0 nM 7.82
CHEMBL302171 Ki = 17.0 nM 7.77
CHEMBL308347 Ki = 22.0 nM 7.66
CHEMBL70589 Ki = 24.0 nM 7.62
CHEMBL306869 Ki = 33.0 nM 7.48
CHEMBL441256 Ki = 65.0 nM 7.19
CHEMBL71899 Ki = 86.0 nM 7.07
CHEMBL302373 Ki = 162.0 nM 6.79
CHEMBL302994 Ki = 177.0 nM 6.75
CHEMBL71395 Ki = 206.0 nM 6.69
CHEMBL303269 Ki = 265.0 nM 6.58
CHEMBL71804 Ki = 419.0 nM 6.38
CHEMBL71319 Ki = 1034.0 nM 5.99