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Assay Detail

CHEMBL4338725

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

Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel Pyrazolyl-dihydroisoquinolines as Positive Allosteric Modulator of the Dopamine D1 Receptor.
Rosse G.
ACS Med Chem Lett (2020) 11 : 4 -4
PubMed 31938453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.15 7.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4464150 1 7.87
CHEMBL4468760 1 7.79
CHEMBL4536851 1 7.74
CHEMBL4449549 1 7.55
CHEMBL4464215 1 7.09
CHEMBL4449550 1 6.95
CHEMBL4590150 1 6.90
CHEMBL4573538 1 6.76
CHEMBL4559891 1 6.54
CHEMBL4465386 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4464150 EC50 = 13.4 nM 7.87
CHEMBL4468760 EC50 = 16.4 nM 7.79
CHEMBL4536851 EC50 = 18.3 nM 7.74
CHEMBL4449549 EC50 = 28.0 nM 7.55
CHEMBL4464215 EC50 = 81.2 nM 7.09
CHEMBL4449550 EC50 = 112.0 nM 6.95
CHEMBL4590150 EC50 = 127.0 nM 6.90
CHEMBL4573538 EC50 = 172.0 nM 6.76
CHEMBL4559891 EC50 = 287.0 nM 6.54
CHEMBL4465386 EC50 = 540.0 nM 6.27