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Assay Detail

CHEMBL1769070

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

Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
7
Total Activities
7
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

Highly potent 5-aminotetrahydropyrazolopyridines: enantioselective dopamine D3 receptor binding, functional selectivity, and analysis of receptor-ligand interactions.
Tschammer N, Elsner J, Goetz A, Ehrlich K, Schuster S, Ruberg M, Kühhorn J, Thompson D, Whistler J, Hübner H, Gmeiner P.
J Med Chem (2011) 54 : 2477 -2491
PubMed 21388142 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.36 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112065 1 7.57
CHEMBL1765629 1 7.23
CHEMBL1765630 1 6.72
CHEMBL1765632 1 6.64
CHEMBL193337 1 6.42
CHEMBL1765631 1 5.20
CHEMBL197159 1 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112065 Ki = 27.0 nM 7.57
CHEMBL1765629 Ki = 59.0 nM 7.23
CHEMBL1765630 Ki = 190.0 nM 6.72
CHEMBL1765632 Ki = 230.0 nM 6.64
CHEMBL193337 Ki = 380.0 nM 6.42
CHEMBL1765631 Ki = 6300.0 nM 5.20
CHEMBL197159 Ki = 17000.0 nM 4.77