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Assay Detail

CHEMBL1949470

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

Binding
Displacement of [3H]-N-methylspiperone from dopamine D3 receptor expressed in human MES-23.5
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol.
Peprah K, Zhu XY, Eyunni SV, Etukala JR, Setola V, Roth BL, Ablordeppey SY.
Bioorg Med Chem (2012) 20 : 1671 -1678
PubMed 22336245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.79 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1946122 1 8.39
CHEMBL1946123 1 8.01
CHEMBL1946745 1 7.89
CHEMBL1946744 1 7.80
CHEMBL1946254 1 6.82
CHEMBL1946126 1 6.68
CHEMBL1946124 1 6.23
CHEMBL1946258 1 6.11
CHEMBL1946255 1 6.06
CHEMBL1946125 1 5.99
CHEMBL1946257 1 5.98
CHEMBL1946253 1 5.52
CHEMBL1946256 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1946122 Ki = 4.1 nM 8.39
CHEMBL1946123 Ki = 9.7 nM 8.01
CHEMBL1946745 Ki = 13.0 nM 7.89
CHEMBL1946744 Ki = 16.0 nM 7.80
CHEMBL1946254 Ki = 152.0 nM 6.82
CHEMBL1946126 Ki = 208.8 nM 6.68
CHEMBL1946124 Ki = 590.0 nM 6.23
CHEMBL1946258 Ki = 777.0 nM 6.11
CHEMBL1946255 Ki = 863.0 nM 6.06
CHEMBL1946125 Ki = 1020.0 nM 5.99
CHEMBL1946257 Ki = 1051.0 nM 5.98
CHEMBL1946253 Ki = 3043.0 nM 5.52
CHEMBL1946256 Ki - -