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Assay Detail

CHEMBL670394

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

Binding
In vitro binding affinity against human D2 dopamine receptor in CHO cells by [3H]spiperone displacement.
19
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.
Sanner MA, Chappie TA, Dunaiskis AR, Fliri AF, Desai KA, Zorn SH, Jackson ER, Johnson CG, Morrone JM, Seymour PA, Majchrzak MJ, Faraci WS, Collins JL, Duignan DB, Prete Di CC, Lee JS, Trozzi A.
Bioorg Med Chem Lett (1998) 8 : 725 -730
PubMed 9871530 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.66 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.08
CHEMBL165504 2 7.42
CHEMBL351611 1 7.36
CHEMBL163009 1 7.17
CHEMBL42 CLOZAPINE 4.0 1 6.81
CHEMBL162265 1 6.73
CHEMBL350160 1 6.73
CHEMBL162873 1 6.71
CHEMBL166321 1 6.69
CHEMBL165113 1 6.59
CHEMBL351098 1 6.04
CHEMBL161899 1 6.02
CHEMBL349699 1 6.01
CHEMBL166269 1 5.94
CHEMBL159903 1 5.92
CHEMBL349904 1 5.76
CHEMBL161982 1 5.73
CHEMBL66227 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.84 nM 9.08
CHEMBL165504 Ki = 38.0 nM 7.42
CHEMBL351611 Ki = 44.0 nM 7.36
CHEMBL165504 Ki = 66.0 nM 7.18
CHEMBL163009 Ki = 68.0 nM 7.17
CHEMBL42 CLOZAPINE Ki = 155.0 nM 6.81
CHEMBL350160 Ki = 187.0 nM 6.73
CHEMBL162265 Ki = 185.0 nM 6.73
CHEMBL162873 Ki = 195.0 nM 6.71
CHEMBL166321 Ki = 206.0 nM 6.69
CHEMBL165113 Ki = 254.0 nM 6.59
CHEMBL351098 Ki = 918.0 nM 6.04
CHEMBL161899 Ki = 948.0 nM 6.02
CHEMBL349699 Ki = 980.0 nM 6.01
CHEMBL166269 Ki = 1140.0 nM 5.94
CHEMBL159903 Ki = 1196.0 nM 5.92
CHEMBL349904 Ki = 1720.0 nM 5.76
CHEMBL161982 Ki = 1880.0 nM 5.73
CHEMBL66227 Ki > 3310.0 nM -