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Assay Detail

CHEMBL4371577

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Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Tan L, Yan W, McCorvy JD, Cheng J.
J Med Chem (2018) 61 : 9841 -9878
PubMed 29939744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 9.20 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1196161 1 9.92
CHEMBL574558 1 9.70
CHEMBL4472022 1 9.52
CHEMBL1193571 1 9.35
CHEMBL35354 1 9.14
CHEMBL288090 1 9.00
CHEMBL286080 SKF-38393 1 8.96
CHEMBL1160787 1 8.70
CHEMBL588 FENOLDOPAM 4.0 1 8.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1196161 EC50 = 0.12 nM 9.92
CHEMBL574558 EC50 = 0.2 nM 9.70
CHEMBL4472022 EC50 = 0.3 nM 9.52
CHEMBL1193571 EC50 = 0.45 nM 9.35
CHEMBL35354 EC50 = 0.73 nM 9.14
CHEMBL288090 EC50 = 1.0 nM 9.00
CHEMBL286080 SKF-38393 EC50 = 1.1 nM 8.96
CHEMBL1160787 EC50 = 2.0 nM 8.70
CHEMBL588 FENOLDOPAM EC50 = 2.8 nM 8.55