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Assay Detail

CHEMBL676134

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

Binding
In vitro low binding affinity towards Dopamine receptor D2 by the displacement of [3H]spiperone radioligand in rat striatal membranes
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

New generation dopaminergic agents. 6. Structure-activity relationship studies of a series of 4-(aminoethoxy)indole and 4-(aminoethoxy)indolone derivatives based on the newly discovered 3-hydroxyphenoxyethylamine D2 template.
Mewshaw RE, Webb MB, Marquis KL, McGaughey GB, Shi X, Wasik T, Scerni R, Brennan JA, Andree TH.
J Med Chem (1999) 42 : 2007 -2020
PubMed 10354409 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.72 8.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61671 1 8.69
CHEMBL435182 1 8.55
CHEMBL60265 1 8.52
CHEMBL292253 1 8.37
CHEMBL305585 1 8.26
CHEMBL303556 1 8.23
CHEMBL62290 1 8.05
CHEMBL59500 1 7.86
CHEMBL64134 1 7.84
CHEMBL59737 1 7.84
CHEMBL304894 1 7.84
CHEMBL294538 1 7.82
CHEMBL64420 1 7.80
CHEMBL300316 1 7.80
CHEMBL60783 1 7.78
CHEMBL294204 1 7.70
CHEMBL59501 1 7.63
CHEMBL60900 1 7.62
CHEMBL60361 1 7.53
CHEMBL60840 1 7.48
CHEMBL64509 1 7.42
CHEMBL64283 1 7.41
CHEMBL61665 1 7.33
CHEMBL64345 1 7.22
CHEMBL64508 1 6.94
CHEMBL64238 1 6.83
CHEMBL302436 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61671 Ki = 2.06 nM 8.69
CHEMBL435182 Ki = 2.8 nM 8.55
CHEMBL60265 Ki = 3.03 nM 8.52
CHEMBL292253 Ki = 4.27 nM 8.37
CHEMBL305585 Ki = 5.5 nM 8.26
CHEMBL303556 Ki = 5.9 nM 8.23
CHEMBL62290 Ki = 9.0 nM 8.05
CHEMBL59500 Ki = 13.8 nM 7.86
CHEMBL64134 Ki = 14.4 nM 7.84
CHEMBL59737 Ki = 14.4 nM 7.84
CHEMBL304894 Ki = 14.6 nM 7.84
CHEMBL294538 Ki = 15.3 nM 7.82
CHEMBL64420 Ki = 15.7 nM 7.80
CHEMBL300316 Ki = 16.0 nM 7.80
CHEMBL60783 Ki = 16.6 nM 7.78
CHEMBL294204 Ki = 19.9 nM 7.70
CHEMBL59501 Ki = 23.4 nM 7.63
CHEMBL60900 Ki = 24.1 nM 7.62
CHEMBL60361 Ki = 29.8 nM 7.53
CHEMBL60840 Ki = 32.9 nM 7.48
CHEMBL64509 Ki = 38.4 nM 7.42
CHEMBL64283 Ki = 39.3 nM 7.41
CHEMBL61665 Ki = 46.7 nM 7.33
CHEMBL64345 Ki = 59.5 nM 7.22
CHEMBL64508 Ki = 115.0 nM 6.94
CHEMBL64238 Ki = 147.0 nM 6.83
CHEMBL302436 Ki = 916.0 nM 6.04