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Assay Detail

CHEMBL861434

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

Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Dopamine/serotonin receptor ligands. 12(1): SAR studies on hexahydro-dibenz[d,g]azecines lead to 4-chloro-7-methyl-5,6,7,8,9,14-hexahydrodibenz[d,g]azecin-3-ol, the first picomolar D5-selective dopamine-receptor antagonist.
Mohr P, Decker M, Enzensperger C, Lehmann J.
J Med Chem (2006) 49 : 2110 -2116
PubMed 16539400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.32 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201170 1 9.41
CHEMBL380464 1 9.34
CHEMBL203637 1 9.08
CHEMBL441618 1 8.72
CHEMBL381936 1 8.70
CHEMBL203047 1 8.51
CHEMBL383451 1 8.49
CHEMBL379662 1 8.12
CHEMBL203689 1 8.06
CHEMBL382010 1 8.05
CHEMBL204065 1 8.03
CHEMBL204098 1 8.03
CHEMBL203734 1 7.60
CHEMBL380330 1 7.54
CHEMBL381946 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201170 Ki = 0.39 nM 9.41
CHEMBL380464 Ki = 0.46 nM 9.34
CHEMBL203637 Ki = 0.83 nM 9.08
CHEMBL441618 Ki = 1.9 nM 8.72
CHEMBL381936 Ki = 2.0 nM 8.70
CHEMBL203047 Ki = 3.1 nM 8.51
CHEMBL383451 Ki = 3.2 nM 8.49
CHEMBL379662 Ki = 7.6 nM 8.12
CHEMBL203689 Ki = 8.7 nM 8.06
CHEMBL382010 Ki = 8.9 nM 8.05
CHEMBL204065 Ki = 9.4 nM 8.03
CHEMBL204098 Ki = 9.3 nM 8.03
CHEMBL203734 Ki = 25.3 nM 7.60
CHEMBL380330 Ki = 28.5 nM 7.54
CHEMBL381946 Ki = 82.0 nM 7.09