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Assay Detail

CHEMBL670990

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Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
10
Total Activities
10
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(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype.
Hübner H, Haubmann C, Utz W, Gmeiner P.
J Med Chem (2000) 43 : 756 -762
PubMed 10691700 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.45 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59 DOPAMINE 4.0 1 8.92
CHEMBL162762 1 7.66
CHEMBL163087 1 6.80
CHEMBL165171 1 5.85
CHEMBL164736 1 5.72
CHEMBL165022 1 5.41
CHEMBL166325 1 4.80
CHEMBL350161 1 -
CHEMBL164631 1 -
CHEMBL164950 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59 DOPAMINE Ki = 1.2 nM 8.92
CHEMBL162762 Ki = 22.0 nM 7.66
CHEMBL163087 Ki = 160.0 nM 6.80
CHEMBL165171 Ki = 1400.0 nM 5.85
CHEMBL164736 Ki = 1900.0 nM 5.72
CHEMBL165022 Ki = 3900.0 nM 5.41
CHEMBL166325 Ki = 16000.0 nM 4.80
CHEMBL350161 Ki > 20000.0 nM -
CHEMBL164631 Ki > 20000.0 nM -
CHEMBL164950 Ki > 20000.0 nM -