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Assay Detail

CHEMBL673447

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Binding
Binding affinity at human Dopamine receptor D3 (hD3) using [3H]spiperone radioligand.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans.
Mewshaw RE, Kavanagh J, Stack G, Marquis KL, Shi X, Kagan MZ, Webb MB, Katz AH, Park A, Kang YH, Abou-Gharbia M, Scerni R, Wasik T, Cortes-Burgos L, Spangler T, Brennan JA, Piesla M, Mazandarani H, Cockett MI, Ochalski R, Coupet J, Andree TH.
J Med Chem (1997) 40 : 4235 -4256
PubMed 9435894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.51 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135044 1 9.70
CHEMBL135725 1 9.00
CHEMBL423890 1 8.96
CHEMBL134807 1 8.62
CHEMBL135357 1 8.47
CHEMBL135395 1 8.08
CHEMBL134343 1 7.71
CHEMBL138016 1 7.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135044 Ki = 0.2 nM 9.70
CHEMBL135725 Ki = 1.0 nM 9.00
CHEMBL423890 Ki = 1.1 nM 8.96
CHEMBL134807 Ki = 2.4 nM 8.62
CHEMBL135357 Ki = 3.4 nM 8.47
CHEMBL135395 Ki = 8.4 nM 8.08
CHEMBL134343 Ki = 19.7 nM 7.71
CHEMBL138016 Ki = 27.6 nM 7.56