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Assay Detail

CHEMBL995089

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

Binding
Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies.
Dörfler M, Tschammer N, Hamperl K, Hübner H, Gmeiner P.
J Med Chem (2008) 51 : 6829 -6838
PubMed 18834111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.41 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58669 1 9.70
CHEMBL484358 1 9.68
CHEMBL484202 1 8.89
CHEMBL483593 1 8.36
CHEMBL485384 1 7.89
CHEMBL485227 1 6.85
CHEMBL491466 1 6.82
CHEMBL59 DOPAMINE 4.0 1 6.62
CHEMBL484203 1 6.55
CHEMBL484357 1 6.52
CHEMBL484204 1 6.02
CHEMBL444128 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58669 Ki = 0.2 nM 9.70
CHEMBL484358 Ki = 0.21 nM 9.68
CHEMBL484202 Ki = 1.3 nM 8.89
CHEMBL483593 Ki = 4.4 nM 8.36
CHEMBL485384 Ki = 13.0 nM 7.89
CHEMBL485227 Ki = 140.0 nM 6.85
CHEMBL491466 Ki = 150.0 nM 6.82
CHEMBL59 DOPAMINE Ki = 240.0 nM 6.62
CHEMBL484203 Ki = 280.0 nM 6.55
CHEMBL484357 Ki = 300.0 nM 6.52
CHEMBL484204 Ki = 950.0 nM 6.02
CHEMBL444128 Ki = 11000.0 nM 4.96