Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL675973

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

Binding
In vitro high binding affinity towards Dopamine receptor D2 by the displacement of [3H]quinpirole radioligand in rat striatal membranes
45
Total Activities
45
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 45 8.74 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303556 1 9.85
CHEMBL60265 1 9.82
CHEMBL64553 1 9.70
CHEMBL59752 1 9.68
CHEMBL61671 1 9.64
CHEMBL64466 1 9.62
CHEMBL300571 1 9.40
CHEMBL435182 1 9.39
CHEMBL64524 1 9.36
CHEMBL292253 1 9.26
CHEMBL60548 1 9.22
CHEMBL62290 1 9.20
CHEMBL63491 1 9.20
CHEMBL305585 1 9.19
CHEMBL59750 1 9.19
CHEMBL64574 1 9.18
CHEMBL434407 1 9.12
CHEMBL304894 1 9.08
CHEMBL418510 1 9.08
CHEMBL291459 1 9.07
CHEMBL418681 1 9.03
CHEMBL59500 1 8.89
CHEMBL302000 1 8.85
CHEMBL60185 1 8.72
CHEMBL64238 1 8.70
CHEMBL300316 1 8.68
CHEMBL59501 1 8.59
CHEMBL60783 1 8.52
CHEMBL60900 1 8.51
CHEMBL64508 1 8.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303556 Ki = 0.14 nM 9.85
CHEMBL60265 Ki = 0.15 nM 9.82
CHEMBL64553 Ki = 0.2 nM 9.70
CHEMBL59752 Ki = 0.21 nM 9.68
CHEMBL61671 Ki = 0.23 nM 9.64
CHEMBL64466 Ki = 0.24 nM 9.62
CHEMBL300571 Ki = 0.4 nM 9.40
CHEMBL435182 Ki = 0.41 nM 9.39
CHEMBL64524 Ki = 0.44 nM 9.36
CHEMBL292253 Ki = 0.55 nM 9.26
CHEMBL60548 Ki = 0.6 nM 9.22
CHEMBL63491 Ki = 0.63 nM 9.20
CHEMBL62290 Ki = 0.63 nM 9.20
CHEMBL305585 Ki = 0.64 nM 9.19
CHEMBL59750 Ki = 0.65 nM 9.19
CHEMBL64574 Ki = 0.66 nM 9.18
CHEMBL434407 Ki = 0.76 nM 9.12
CHEMBL304894 Ki = 0.84 nM 9.08
CHEMBL418510 Ki = 0.84 nM 9.08
CHEMBL291459 Ki = 0.86 nM 9.07
CHEMBL418681 Ki = 0.93 nM 9.03
CHEMBL59500 Ki = 1.3 nM 8.89
CHEMBL302000 Ki = 1.4 nM 8.85
CHEMBL60185 Ki = 1.9 nM 8.72
CHEMBL64238 Ki = 2.0 nM 8.70
CHEMBL300316 Ki = 2.08 nM 8.68
CHEMBL59501 Ki = 2.6 nM 8.59
CHEMBL60783 Ki = 3.0 nM 8.52
CHEMBL60900 Ki = 3.1 nM 8.51
CHEMBL64508 Ki = 3.6 nM 8.44
CHEMBL64420 Ki = 4.8 nM 8.32
CHEMBL64798 Ki = 4.8 nM 8.32
CHEMBL59737 Ki = 5.3 nM 8.28
CHEMBL294538 Ki = 6.34 nM 8.20
CHEMBL59992 Ki = 6.7 nM 8.17
CHEMBL416856 Ki = 6.93 nM 8.16
CHEMBL294204 Ki = 7.0 nM 8.15
CHEMBL64134 Ki = 7.4 nM 8.13
CHEMBL64283 Ki = 9.7 nM 8.01
CHEMBL302436 Ki = 12.1 nM 7.92
CHEMBL64509 Ki = 12.3 nM 7.91
CHEMBL61665 Ki = 17.4 nM 7.76
CHEMBL60840 Ki = 30.3 nM 7.52
CHEMBL64345 Ki = 50.0 nM 7.30
CHEMBL60361 Ki = 77.1 nM 7.11