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Assay Detail

CHEMBL1769066

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

Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Tissue Cerebral cortex
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(1A) dopamine receptor (CHEMBL5067)
Type SINGLE PROTEIN
Organism Sus scrofa

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 5.10 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112065 1 6.24
CHEMBL1765632 1 5.75
CHEMBL1765630 1 5.44
CHEMBL1765629 1 5.17
CHEMBL1765631 1 4.64
CHEMBL193337 1 4.28
CHEMBL197159 1 4.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112065 Ki = 570.0 nM 6.24
CHEMBL1765632 Ki = 1800.0 nM 5.75
CHEMBL1765630 Ki = 3600.0 nM 5.44
CHEMBL1765629 Ki = 6800.0 nM 5.17
CHEMBL1765631 Ki = 23000.0 nM 4.64
CHEMBL193337 Ki = 53000.0 nM 4.28
CHEMBL197159 Ki = 68000.0 nM 4.17