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Assay Detail

CHEMBL673083

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Binding
In vitro binding affinity at human Dopamine receptor D2 (long) by [3H]spiroperidol displacement.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand.
Perrone R, Berardi F, Colabufo NA, Leopoldo M, Tortorella V.
J Med Chem (2000) 43 : 270 -277
PubMed 10649982 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 5.73 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL328283 1 6.58
CHEMBL329228 1 6.55
CHEMBL420067 1 6.01
CHEMBL93403 1 5.72
CHEMBL315879 1 5.63
CHEMBL327245 1 5.59
CHEMBL318747 1 5.56
CHEMBL2112375 1 5.50
CHEMBL321557 1 5.47
CHEMBL92713 1 5.40
CHEMBL330470 1 5.40
CHEMBL96462 1 5.30
CHEMBL92121 1 -
CHEMBL96322 1 -
CHEMBL92411 1 -
CHEMBL94265 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL328283 Ki = 262.0 nM 6.58
CHEMBL329228 Ki = 282.0 nM 6.55
CHEMBL420067 Ki = 980.0 nM 6.01
CHEMBL93403 Ki = 1900.0 nM 5.72
CHEMBL315879 Ki = 2350.0 nM 5.63
CHEMBL327245 Ki = 2550.0 nM 5.59
CHEMBL318747 Ki = 2740.0 nM 5.56
CHEMBL2112375 Ki = 3180.0 nM 5.50
CHEMBL321557 Ki = 3400.0 nM 5.47
CHEMBL92713 Ki = 3950.0 nM 5.40
CHEMBL330470 Ki = 3960.0 nM 5.40
CHEMBL96462 Ki = 5000.0 nM 5.30
CHEMBL92121 Ki > 850.0 nM -
CHEMBL96322 Ki > 850.0 nM -
CHEMBL92411 Ki > 850.0 nM -
CHEMBL94265 Ki > 850.0 nM -