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Assay Detail

CHEMBL1044815

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Functional
Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

D(1A) dopamine receptor (CHEMBL2056)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

'Click' D(1) receptor agonists with a 5-HT(1A) receptor pharmacophore producing D(2) receptor activity.
Zhang J, Zhang H, Cai W, Yu L, Zhen X, Zhang A.
Bioorg Med Chem (2009) 17 : 4873 -4880
PubMed 19559623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Imax 2 - -
IC50 2 4.60 4.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL574700 2 4.70
CHEMBL582945 2 4.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL574700 IC50 = 19800.0 nM 4.70
CHEMBL582945 IC50 = 32700.0 nM 4.49
CHEMBL582945 Imax = 100.0 % -
CHEMBL574700 Imax = 70.0 % -