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Assay Detail

CHEMBL861438

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

Binding
Binding affinity to D5 dopamine receptor by radioligand binding assay
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(1B) dopamine receptor (CHEMBL1850)
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 8.35 10.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203637 1 10.24
CHEMBL380464 1 9.01
CHEMBL201170 1 8.82
CHEMBL381936 1 8.78
CHEMBL203047 1 8.31
CHEMBL441618 1 8.12
CHEMBL204065 1 7.90
CHEMBL382010 1 7.37
CHEMBL204098 1 6.64
CHEMBL379662 1 -
CHEMBL203689 1 -
CHEMBL203734 1 -
CHEMBL381946 1 -
CHEMBL383451 1 -
CHEMBL380330 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203637 Ki = 0.057 nM 10.24
CHEMBL380464 Ki = 0.98 nM 9.01
CHEMBL201170 Ki = 1.5 nM 8.82
CHEMBL381936 Ki = 1.68 nM 8.78
CHEMBL203047 Ki = 4.9 nM 8.31
CHEMBL441618 Ki = 7.5 nM 8.12
CHEMBL204065 Ki = 12.6 nM 7.90
CHEMBL382010 Ki = 42.3 nM 7.37
CHEMBL204098 Ki = 226.5 nM 6.64
CHEMBL379662 Ki - -
CHEMBL203689 Ki - -
CHEMBL203734 Ki - -
CHEMBL381946 Ki - -
CHEMBL383451 Ki - -
CHEMBL380330 Ki - -