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Assay Detail

CHEMBL995090

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

Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cells
11
Total Activities
11
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(4) dopamine receptor (CHEMBL219)
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 11 6.54 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL484358 1 8.37
CHEMBL59 DOPAMINE 4.0 1 8.21
CHEMBL483593 1 7.16
CHEMBL484203 1 7.00
CHEMBL484202 1 6.72
CHEMBL485227 1 6.17
CHEMBL491466 1 5.96
CHEMBL484204 1 5.85
CHEMBL485384 1 5.75
CHEMBL484357 1 5.51
CHEMBL444128 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL484358 Ki = 4.3 nM 8.37
CHEMBL59 DOPAMINE Ki = 6.2 nM 8.21
CHEMBL483593 Ki = 69.0 nM 7.16
CHEMBL484203 Ki = 100.0 nM 7.00
CHEMBL484202 Ki = 190.0 nM 6.72
CHEMBL485227 Ki = 670.0 nM 6.17
CHEMBL491466 Ki = 1100.0 nM 5.96
CHEMBL484204 Ki = 1400.0 nM 5.85
CHEMBL485384 Ki = 1800.0 nM 5.75
CHEMBL484357 Ki = 3100.0 nM 5.51
CHEMBL444128 Ki = 6100.0 nM 5.21