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Assay Detail

CHEMBL673594

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Binding
In vitro binding affinity to rat striatal Dopamine receptor D2 was determined using the agonist [3H]quinpirole to label the high affinity state (D2 high)
ChEMBL ↗
62
Total Activities
62
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 62 8.57 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134489 — — 1 9.70
CHEMBL134807 — — 1 9.70
CHEMBL135395 — — 1 9.70
CHEMBL134930 — — 1 9.52
CHEMBL135201 — — 1 9.52
CHEMBL135873 — — 1 9.52
CHEMBL136635 — — 1 9.52
CHEMBL134677 — — 1 9.40
CHEMBL423890 — — 1 9.40
CHEMBL135495 — — 1 9.40
CHEMBL134448 — — 1 9.30
CHEMBL134725 — — 1 9.30
CHEMBL334616 — — 1 9.30
CHEMBL135183 — — 1 9.30
CHEMBL134808 — — 1 9.22
CHEMBL135357 — — 1 9.22
CHEMBL135044 — — 1 9.22
CHEMBL134663 — — 1 9.22
CHEMBL339190 — — 1 9.22
CHEMBL337724 — — 1 9.22
CHEMBL135222 — — 1 9.15
CHEMBL424087 — — 1 9.15
CHEMBL134707 — — 1 9.15
CHEMBL334406 — — 1 9.10
CHEMBL135546 — — 1 9.10
CHEMBL543426 — — 1 9.05
CHEMBL336390 — — 1 9.05
CHEMBL135137 — — 1 9.05
CHEMBL135752 — — 1 9.00
CHEMBL337228 — — 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134489 — Ki = 0.2 nM 9.70
CHEMBL134807 — Ki = 0.2 nM 9.70
CHEMBL135395 — Ki = 0.2 nM 9.70
CHEMBL134930 — Ki = 0.3 nM 9.52
CHEMBL135201 — Ki = 0.3 nM 9.52
CHEMBL135873 — Ki = 0.3 nM 9.52
CHEMBL136635 — Ki = 0.3 nM 9.52
CHEMBL135495 — Ki = 0.4 nM 9.40
CHEMBL134677 — Ki = 0.4 nM 9.40
CHEMBL423890 — Ki = 0.4 nM 9.40
CHEMBL135183 — Ki = 0.5 nM 9.30
CHEMBL334616 — Ki = 0.5 nM 9.30
CHEMBL134725 — Ki = 0.5 nM 9.30
CHEMBL134448 — Ki = 0.5 nM 9.30
CHEMBL337724 — Ki = 0.6 nM 9.22
CHEMBL134808 — Ki = 0.6 nM 9.22
CHEMBL339190 — Ki = 0.6 nM 9.22
CHEMBL134663 — Ki = 0.6 nM 9.22
CHEMBL135044 — Ki = 0.6 nM 9.22
CHEMBL135357 — Ki = 0.6 nM 9.22
CHEMBL135222 — Ki = 0.7 nM 9.15
CHEMBL424087 — Ki = 0.7 nM 9.15
CHEMBL134707 — Ki = 0.7 nM 9.15
CHEMBL334406 — Ki = 0.8 nM 9.10
CHEMBL135546 — Ki = 0.8 nM 9.10
CHEMBL543426 — Ki = 0.9 nM 9.05
CHEMBL135137 — Ki = 0.9 nM 9.05
CHEMBL336390 — Ki = 0.9 nM 9.05
CHEMBL135752 — Ki = 1.0 nM 9.00
CHEMBL337228 — Ki = 1.0 nM 9.00
CHEMBL134582 — Ki = 1.1 nM 8.96
CHEMBL135242 — Ki = 1.1 nM 8.96
CHEMBL135285 — Ki = 1.1 nM 8.96
CHEMBL340267 — Ki = 1.2 nM 8.92
CHEMBL134605 — Ki = 1.2 nM 8.92
CHEMBL134843 — Ki = 1.6 nM 8.80
CHEMBL134281 — Ki = 2.3 nM 8.64
CHEMBL135116 — Ki = 2.4 nM 8.62
CHEMBL336856 — Ki = 3.4 nM 8.47
CHEMBL135291 — Ki = 4.8 nM 8.32
CHEMBL279085 TALIPEXOLE Ki = 5.8 nM 8.24
CHEMBL135636 — Ki = 6.9 nM 8.16
CHEMBL133367 — Ki = 7.1 nM 8.15
CHEMBL135269 — Ki = 7.9 nM 8.10
CHEMBL337696 — Ki = 8.8 nM 8.06
CHEMBL138016 — Ki = 12.0 nM 7.92
CHEMBL423335 — Ki = 13.1 nM 7.88
CHEMBL133833 — Ki = 16.0 nM 7.80
CHEMBL7549 PRECLAMOL Ki = 21.4 nM 7.67
CHEMBL135011 — Ki = 22.0 nM 7.66