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Assay Detail

CHEMBL673595

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Binding
In vitro binding affinity to rat striatal Dopamine receptor D2 was determined using the antagonist [3H]spiperone + GTP to label the low affinity state (D2 low)
ChEMBL ↗
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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. 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 60 7.41 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL336390 — — 1 9.00
CHEMBL135357 — — 1 8.66
CHEMBL337724 — — 1 8.55
CHEMBL134489 — — 1 8.55
CHEMBL134808 — — 1 8.49
CHEMBL134807 — — 1 8.48
CHEMBL135242 — — 1 8.42
CHEMBL135044 — — 1 8.42
CHEMBL134663 — — 1 8.40
CHEMBL423890 — — 1 8.24
CHEMBL134448 — — 1 8.17
CHEMBL337228 — — 1 8.15
CHEMBL135137 — — 1 8.14
CHEMBL135395 — — 1 8.08
CHEMBL134930 — — 1 7.99
CHEMBL134677 — — 1 7.94
CHEMBL135183 — — 1 7.92
CHEMBL134707 — — 1 7.89
CHEMBL424087 — — 1 7.87
CHEMBL135495 — — 1 7.87
CHEMBL334616 — — 1 7.84
CHEMBL543426 — — 1 7.80
CHEMBL339190 — — 1 7.79
CHEMBL135201 — — 1 7.79
CHEMBL135222 — — 1 7.77
CHEMBL136635 — — 1 7.75
CHEMBL134725 — — 1 7.74
CHEMBL134605 — — 1 7.71
CHEMBL135752 — — 1 7.62
CHEMBL133367 — — 1 7.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL336390 — Ki = 1.0 nM 9.00
CHEMBL135357 — Ki = 2.2 nM 8.66
CHEMBL134489 — Ki = 2.8 nM 8.55
CHEMBL337724 — Ki = 2.8 nM 8.55
CHEMBL134808 — Ki = 3.2 nM 8.49
CHEMBL134807 — Ki = 3.3 nM 8.48
CHEMBL135242 — Ki = 3.8 nM 8.42
CHEMBL135044 — Ki = 3.8 nM 8.42
CHEMBL134663 — Ki = 4.0 nM 8.40
CHEMBL423890 — Ki = 5.7 nM 8.24
CHEMBL134448 — Ki = 6.7 nM 8.17
CHEMBL337228 — Ki = 7.1 nM 8.15
CHEMBL135137 — Ki = 7.2 nM 8.14
CHEMBL135395 — Ki = 8.4 nM 8.08
CHEMBL134930 — Ki = 10.3 nM 7.99
CHEMBL134677 — Ki = 11.4 nM 7.94
CHEMBL135183 — Ki = 12.0 nM 7.92
CHEMBL134707 — Ki = 13.0 nM 7.89
CHEMBL424087 — Ki = 13.4 nM 7.87
CHEMBL135495 — Ki = 13.5 nM 7.87
CHEMBL334616 — Ki = 14.6 nM 7.84
CHEMBL543426 — Ki = 15.9 nM 7.80
CHEMBL339190 — Ki = 16.2 nM 7.79
CHEMBL135201 — Ki = 16.2 nM 7.79
CHEMBL135222 — Ki = 17.0 nM 7.77
CHEMBL136635 — Ki = 17.8 nM 7.75
CHEMBL134725 — Ki = 18.4 nM 7.74
CHEMBL134605 — Ki = 19.4 nM 7.71
CHEMBL135752 — Ki = 24.1 nM 7.62
CHEMBL133367 — Ki = 25.4 nM 7.59
CHEMBL135546 — Ki = 26.4 nM 7.58
CHEMBL134281 — Ki = 26.9 nM 7.57
CHEMBL134343 — Ki = 28.1 nM 7.55
CHEMBL135873 — Ki = 32.4 nM 7.49
CHEMBL134843 — Ki = 36.0 nM 7.44
CHEMBL134582 — Ki = 42.0 nM 7.38
CHEMBL340267 — Ki = 44.0 nM 7.36
CHEMBL337696 — Ki = 46.3 nM 7.33
CHEMBL135291 — Ki = 61.1 nM 7.21
CHEMBL135116 — Ki = 62.0 nM 7.21
CHEMBL334406 — Ki = 68.9 nM 7.16
CHEMBL135636 — Ki = 96.0 nM 7.02
CHEMBL133833 — Ki = 102.0 nM 6.99
CHEMBL135725 — Ki = 110.0 nM 6.96
CHEMBL138016 — Ki = 110.0 nM 6.96
CHEMBL135285 — Ki = 115.0 nM 6.94
CHEMBL336856 — Ki = 177.0 nM 6.75
CHEMBL135011 — Ki = 230.0 nM 6.64
CHEMBL423335 — Ki = 278.0 nM 6.56
CHEMBL135269 — Ki = 372.0 nM 6.43