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Assay Detail

CHEMBL5104730

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

Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Synthesis and Preclinical Characterization of LY3154885, a Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Nonclinical Drug-Drug Interaction Risk Profile.
Hao J, Beck J, Zhou X, Lackner GL, Johnston R, Reinhard M, Goldsmith P, Hollinshead S, Dehlinger V, Filla SA, Wang XS, Richardson J, Posada M, Mohutsky M, Schober D, Katner JS, Chen Q, Hu B, Remick DM, Coates DA, Mathes BM, Hawk MK, Svensson KA, Hembre E.
J Med Chem (2022) 65 : 3786 -3797
PubMed 35175768 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.90 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4464150 1 8.19
CHEMBL4559891 1 7.99
CHEMBL4468760 1 7.93
CHEMBL4573538 1 7.80
CHEMBL5187909 1 7.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4464150 EC50 = 6.41 nM 8.19
CHEMBL4559891 EC50 = 10.3 nM 7.99
CHEMBL4468760 EC50 = 11.7 nM 7.93
CHEMBL4573538 EC50 = 15.9 nM 7.80
CHEMBL5187909 EC50 = 25.6 nM 7.59