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Assay Detail

CHEMBL858784

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

Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
44
Total Activities
44
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 Expert

Target

D(1B) dopamine receptor (CHEMBL1850)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dopamine/serotonin receptor ligands. 10: SAR Studies on azecine-type dopamine receptor ligands by functional screening at human cloned D1, D2L, and D5 receptors with a microplate reader based calcium assay lead to a novel potent D1/D5 selective antagonist.
Hoefgen B, Decker M, Mohr P, Schramm AM, Rostom SA, El-Subbagh H, Schweikert PM, Rudolf DR, Kassack MU, Lehmann J.
J Med Chem (2006) 49 : 760 -769
PubMed 16420061 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 44 6.97 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1204122 1 8.82
CHEMBL201525 1 7.95
CHEMBL382850 1 7.83
CHEMBL201093 1 7.10
CHEMBL201483 1 6.44
CHEMBL201432 1 6.05
CHEMBL1202298 1 5.97
CHEMBL202924 1 5.58
CHEMBL379450 1 -
CHEMBL201288 1 -
CHEMBL381573 1 -
CHEMBL440390 1 -
CHEMBL426662 1 -
CHEMBL381102 1 -
CHEMBL379673 1 -
CHEMBL201142 1 -
CHEMBL201177 1 -
CHEMBL345349 1 -
CHEMBL201287 1 -
CHEMBL201577 1 -
CHEMBL382780 1 -
CHEMBL201575 1 -
CHEMBL201086 1 -
CHEMBL381912 1 -
CHEMBL201748 1 -
CHEMBL201444 1 -
CHEMBL378358 1 -
CHEMBL380484 1 -
CHEMBL201334 1 -
CHEMBL201241 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1204122 Ki = 1.5 nM 8.82
CHEMBL201525 Ki = 11.2 nM 7.95
CHEMBL382850 Ki = 14.7 nM 7.83
CHEMBL201093 Ki = 79.1 nM 7.10
CHEMBL201483 Ki = 361.0 nM 6.44
CHEMBL201432 Ki = 893.0 nM 6.05
CHEMBL1202298 Ki = 1078.0 nM 5.97
CHEMBL202924 Ki = 2610.0 nM 5.58
CHEMBL201177 Ki - -
CHEMBL380124 Ki - -
CHEMBL345349 Ki - -
CHEMBL201287 Ki - -
CHEMBL201288 Ki - -
CHEMBL201010 Ki - -
CHEMBL383102 Ki - -
CHEMBL201598 Ki - -
CHEMBL201375 Ki - -
CHEMBL201788 Ki - -
CHEMBL437888 Ki - -
CHEMBL381325 Ki - -
CHEMBL201561 Ki - -
CHEMBL381472 Ki - -
CHEMBL382642 Ki - -
CHEMBL1398 ALPHA-PHENYL-GAMMA-BUTYROLACTONE Ki - -
CHEMBL201739 Ki - -
CHEMBL201393 Ki - -
CHEMBL201575 Ki - -
CHEMBL201241 Ki - -
CHEMBL201334 Ki - -
CHEMBL380484 Ki - -
CHEMBL378358 Ki - -
CHEMBL201444 Ki - -
CHEMBL201748 Ki - -
CHEMBL381912 Ki - -
CHEMBL201086 Ki - -
CHEMBL201142 Ki - -
CHEMBL382780 Ki - -
CHEMBL201577 Ki - -
CHEMBL379450 Ki - -
CHEMBL381573 Ki - -
CHEMBL440390 Ki - -
CHEMBL426662 Ki - -
CHEMBL381102 Ki - -
CHEMBL379673 Ki - -