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Assay Detail

CHEMBL671375

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

Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D2 stably expressed in CHO cell lines
32
Total Activities
32
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

1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels.
Carling RW, Moore KW, Moyes CR, Jones EA, Bonner K, Emms F, Marwood R, Patel S, Patel S, Fletcher AE, Beer M, Sohal B, Pike A, Leeson PD.
J Med Chem (1999) 42 : 2706 -2715
PubMed 10411491 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 7.05 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL90005 1 8.11
CHEMBL93432 1 8.06
CHEMBL91669 1 7.96
CHEMBL328739 1 7.82
CHEMBL91498 1 7.58
CHEMBL89971 1 7.42
CHEMBL263162 1 7.28
CHEMBL91162 1 7.25
CHEMBL93969 1 7.22
CHEMBL94283 1 7.14
CHEMBL42 CLOZAPINE 4.0 1 7.13
CHEMBL93958 1 7.09
CHEMBL316125 1 7.08
CHEMBL91621 1 7.07
CHEMBL92859 1 7.02
CHEMBL450021 1 6.96
CHEMBL328667 1 6.82
CHEMBL94023 1 6.77
CHEMBL91272 1 6.72
CHEMBL91229 1 6.66
CHEMBL91553 1 6.57
CHEMBL91821 1 6.55
CHEMBL92189 1 6.54
CHEMBL327176 1 6.48
CHEMBL91155 1 6.05
CHEMBL93832 1 5.89
CHEMBL93970 1 -
CHEMBL327339 1 -
CHEMBL431095 1 -
CHEMBL90711 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL90005 Ki = 7.8 nM 8.11
CHEMBL93432 Ki = 8.8 nM 8.06
CHEMBL91669 Ki = 11.0 nM 7.96
CHEMBL328739 Ki = 15.0 nM 7.82
CHEMBL91498 Ki = 26.0 nM 7.58
CHEMBL89971 Ki = 38.0 nM 7.42
CHEMBL263162 Ki = 52.0 nM 7.28
CHEMBL91162 Ki = 56.0 nM 7.25
CHEMBL93969 Ki = 60.0 nM 7.22
CHEMBL94283 Ki = 73.0 nM 7.14
CHEMBL42 CLOZAPINE Ki = 74.0 nM 7.13
CHEMBL93958 Ki = 82.0 nM 7.09
CHEMBL316125 Ki = 83.0 nM 7.08
CHEMBL91621 Ki = 86.0 nM 7.07
CHEMBL92859 Ki = 95.0 nM 7.02
CHEMBL450021 Ki = 110.0 nM 6.96
CHEMBL328667 Ki = 150.0 nM 6.82
CHEMBL94023 Ki = 170.0 nM 6.77
CHEMBL91272 Ki = 190.0 nM 6.72
CHEMBL91229 Ki = 220.0 nM 6.66
CHEMBL91553 Ki = 270.0 nM 6.57
CHEMBL91821 Ki = 280.0 nM 6.55
CHEMBL92189 Ki = 290.0 nM 6.54
CHEMBL327176 Ki = 330.0 nM 6.48
CHEMBL91155 Ki = 900.0 nM 6.05
CHEMBL93832 Ki = 1300.0 nM 5.89
CHEMBL93970 Ki > 1500.0 nM -
CHEMBL327339 Ki > 1600.0 nM -
CHEMBL431095 Ki > 1900.0 nM -
CHEMBL90711 Ki > 1600.0 nM -
CHEMBL327310 Ki > 1700.0 nM -
CHEMBL444309 Ki > 1700.0 nM -