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Assay Detail

CHEMBL995091

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

Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Tissue Striatum
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

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 10 5.28 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL491466 1 5.77
CHEMBL484358 1 5.54
CHEMBL483593 1 5.42
CHEMBL485227 1 5.34
CHEMBL485384 1 5.24
CHEMBL484204 1 5.17
CHEMBL444128 1 5.14
CHEMBL484202 1 5.02
CHEMBL484357 1 4.89
CHEMBL484203 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL491466 Ki = 1700.0 nM 5.77
CHEMBL484358 Ki = 2900.0 nM 5.54
CHEMBL483593 Ki = 3800.0 nM 5.42
CHEMBL485227 Ki = 4600.0 nM 5.34
CHEMBL485384 Ki = 5800.0 nM 5.24
CHEMBL484204 Ki = 6800.0 nM 5.17
CHEMBL444128 Ki = 7300.0 nM 5.14
CHEMBL484202 Ki = 9500.0 nM 5.02
CHEMBL484357 Ki = 13000.0 nM 4.89
CHEMBL484203 Ki > 100000.0 nM -