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Assay Detail

CHEMBL4409080

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

Binding
Displacement of [3H]-spiperone from human D3 receptor expressed in CHO cells co-expressing Galpha16 incubated for 120 mins by liquid scintillation counting method
22
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems.
Grillo A, Chemi G, Brogi S, Brindisi M, Relitti N, Fezza F, Fazio D, Castelletti L, Perdona E, Wong A, Lamponi S, Pecorelli A, Benedusi M, Fantacci M, Valoti M, Valacchi G, Micheli F, Novellino E, Campiani G, Butini S, Maccarrone M, Gemma S.
Eur J Med Chem (2019) 183 : 111674 -111674
PubMed 31518969 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.18 7.72
pKi 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4540218 2 7.72
CHEMBL4554053 2 7.47
CHEMBL4517296 2 7.12
CHEMBL4473519 2 6.98
CHEMBL4471658 2 6.98
CHEMBL4565200 2 6.83
CHEMBL184238 URB-597 1.0 2 -
CHEMBL4446507 2 -
CHEMBL4520982 2 -
CHEMBL4449756 2 -
CHEMBL4520184 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4540218 Ki = 19.0 nM 7.72
CHEMBL4540218 Ki = 19.5 nM 7.71
CHEMBL4554053 Ki = 33.88 nM 7.47
CHEMBL4554053 Ki = 34.0 nM 7.47
CHEMBL4517296 Ki = 75.86 nM 7.12
CHEMBL4517296 Ki = 76.0 nM 7.12
CHEMBL4473519 Ki = 105.0 nM 6.98
CHEMBL4471658 Ki = 104.71 nM 6.98
CHEMBL4473519 Ki = 104.71 nM 6.98
CHEMBL4471658 Ki = 105.0 nM 6.98
CHEMBL4565200 Ki = 147.91 nM 6.83
CHEMBL4565200 Ki = 148.0 nM 6.83
CHEMBL4520184 Ki - -
CHEMBL4449756 Ki - -
CHEMBL184238 URB-597 pKi - -
CHEMBL4520982 Ki - -
CHEMBL4446507 pKi - -
CHEMBL4520982 pKi - -
CHEMBL4449756 pKi - -
CHEMBL4520184 pKi - -
CHEMBL4446507 Ki - -
CHEMBL184238 URB-597 Ki - -