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Assay Detail

CHEMBL3801475

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

Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
14
Total Activities
14
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

Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.
Weichert D, Stanek M, Hübner H, Gmeiner P.
Bioorg Med Chem (2016) 24 : 2641 -2653
PubMed 27132867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.75 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3797758 1 6.68
CHEMBL3800303 1 6.37
CHEMBL3799593 1 6.37
CHEMBL3800636 1 6.07
CHEMBL3797876 1 6.05
CHEMBL3800341 1 6.02
CHEMBL3799455 1 5.55
CHEMBL3797205 1 5.55
CHEMBL3799427 1 5.54
CHEMBL3798748 1 5.35
CHEMBL3800468 1 5.17
CHEMBL240773 QUINPIROLE 2.0 1 5.06
CHEMBL3800400 1 4.96
CHEMBL434 ISOPROTERENOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3797758 Ki = 210.0 nM 6.68
CHEMBL3800303 Ki = 430.0 nM 6.37
CHEMBL3799593 Ki = 430.0 nM 6.37
CHEMBL3800636 Ki = 860.0 nM 6.07
CHEMBL3797876 Ki = 890.0 nM 6.05
CHEMBL3800341 Ki = 960.0 nM 6.02
CHEMBL3799455 Ki = 2800.0 nM 5.55
CHEMBL3797205 Ki = 2800.0 nM 5.55
CHEMBL3799427 Ki = 2900.0 nM 5.54
CHEMBL3798748 Ki = 4500.0 nM 5.35
CHEMBL3800468 Ki = 6800.0 nM 5.17
CHEMBL240773 QUINPIROLE Ki = 8700.0 nM 5.06
CHEMBL3800400 Ki = 11000.0 nM 4.96
CHEMBL434 ISOPROTERENOL Ki > 50000.0 nM -