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Assay Detail

CHEMBL670415

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

Binding
Ability to displace [3H]spiperone from D2 dopamine receptor isolated from the striata of male Wistar rats
26
Total Activities
26
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 (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-(2-pyrrolidinylmethyl)benzoxazine-8-carboxamides exhibiting high affinities for All of D2, 5-HT1 A, and 5-HT2 receptors
Kuroita T, Ikebe T, Murakami S, Takehara S, Kawakita T
Bioorg Med Chem Lett (1995) 5 : 1245 -1250
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.54 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.82
CHEMBL85 RISPERIDONE 4.0 1 8.74
CHEMBL21971 1 8.44
CHEMBL22772 1 8.42
CHEMBL278151 1 8.38
CHEMBL21802 1 8.19
CHEMBL21819 1 7.80
CHEMBL21318 1 7.77
CHEMBL22306 1 7.72
CHEMBL279937 1 7.24
CHEMBL278838 1 7.08
CHEMBL21940 1 7.04
CHEMBL280912 1 6.75
CHEMBL22468 1 6.68
CHEMBL22835 1 6.57
CHEMBL21386 1 6.51
CHEMBL281363 1 6.10
CHEMBL279292 1 -
CHEMBL21680 1 -
CHEMBL21403 1 -
CHEMBL418374 1 -
CHEMBL22154 1 -
CHEMBL418560 1 -
CHEMBL282935 1 -
CHEMBL279698 1 -
CHEMBL22469 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 1.5 nM 8.82
CHEMBL85 RISPERIDONE Ki = 1.8 nM 8.74
CHEMBL21971 Ki = 3.6 nM 8.44
CHEMBL22772 Ki = 3.8 nM 8.42
CHEMBL278151 Ki = 4.2 nM 8.38
CHEMBL21802 Ki = 6.5 nM 8.19
CHEMBL21819 Ki = 16.0 nM 7.80
CHEMBL21318 Ki = 17.0 nM 7.77
CHEMBL22306 Ki = 19.0 nM 7.72
CHEMBL279937 Ki = 57.0 nM 7.24
CHEMBL278838 Ki = 84.0 nM 7.08
CHEMBL21940 Ki = 92.0 nM 7.04
CHEMBL280912 Ki = 180.0 nM 6.75
CHEMBL22468 Ki = 210.0 nM 6.68
CHEMBL22835 Ki = 270.0 nM 6.57
CHEMBL21386 Ki = 310.0 nM 6.51
CHEMBL281363 Ki = 800.0 nM 6.10
CHEMBL279292 Ki > 1000.0 nM -
CHEMBL21680 Ki > 1000.0 nM -
CHEMBL21403 Ki > 1000.0 nM -
CHEMBL418374 Ki > 1000.0 nM -
CHEMBL22154 Ki > 1000.0 nM -
CHEMBL418560 Ki > 1000.0 nM -
CHEMBL282935 Ki > 1000.0 nM -
CHEMBL279698 Ki > 1000.0 nM -
CHEMBL22469 Ki > 1000.0 nM -