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Assay Detail

CHEMBL2390228

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

Binding
Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum after 15 mins by liquid scintillation counting analysis
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
Chen Y, Wang S, Xu X, Liu X, Yu M, Zhao S, Liu S, Qiu Y, Zhang T, Liu BF, Zhang G.
J Med Chem (2013) 56 : 4671 -4690
PubMed 23675993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 45 6.85 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2387253 1 8.85
CHEMBL2387229 1 8.59
CHEMBL85 RISPERIDONE 4.0 1 8.43
CHEMBL2387245 1 8.41
CHEMBL2385102 1 8.40
CHEMBL2387260 1 8.31
CHEMBL2387230 1 8.28
CHEMBL2387233 1 7.97
CHEMBL2387265 1 7.83
CHEMBL2387239 1 7.77
CHEMBL2387249 1 7.35
CHEMBL2387237 1 6.93
CHEMBL2387227 1 6.92
CHEMBL2387238 1 6.91
CHEMBL42 CLOZAPINE 4.0 1 6.89
CHEMBL2387256 1 6.85
CHEMBL2387254 1 6.81
CHEMBL2387259 1 6.75
CHEMBL2387251 1 6.74
CHEMBL2387262 1 6.62
CHEMBL2387255 1 6.38
CHEMBL2387232 1 6.34
CHEMBL2387242 1 6.29
CHEMBL2387250 1 6.25
CHEMBL2387234 1 6.20
CHEMBL2387235 1 6.10
CHEMBL2387228 1 6.07
CHEMBL2387241 1 6.01
CHEMBL2387257 1 5.86
CHEMBL2387252 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2387253 Ki = 1.4 nM 8.85
CHEMBL2387229 Ki = 2.6 nM 8.59
CHEMBL85 RISPERIDONE Ki = 3.7 nM 8.43
CHEMBL2387245 Ki = 3.9 nM 8.41
CHEMBL2385102 Ki = 4.0 nM 8.40
CHEMBL2387260 Ki = 4.9 nM 8.31
CHEMBL2387230 Ki = 5.3 nM 8.28
CHEMBL2387233 Ki = 10.7 nM 7.97
CHEMBL2387265 Ki = 14.8 nM 7.83
CHEMBL2387239 Ki = 17.1 nM 7.77
CHEMBL2387249 Ki = 44.9 nM 7.35
CHEMBL2387237 Ki = 116.3 nM 6.93
CHEMBL2387227 Ki = 119.1 nM 6.92
CHEMBL2387238 Ki = 122.8 nM 6.91
CHEMBL42 CLOZAPINE Ki = 128.7 nM 6.89
CHEMBL2387256 Ki = 142.6 nM 6.85
CHEMBL2387254 Ki = 156.3 nM 6.81
CHEMBL2387259 Ki = 176.3 nM 6.75
CHEMBL2387251 Ki = 182.4 nM 6.74
CHEMBL2387262 Ki = 241.9 nM 6.62
CHEMBL2387255 Ki = 412.1 nM 6.38
CHEMBL2387232 Ki = 459.3 nM 6.34
CHEMBL2387242 Ki = 515.2 nM 6.29
CHEMBL2387250 Ki = 568.7 nM 6.25
CHEMBL2387234 Ki = 631.6 nM 6.20
CHEMBL2387235 Ki = 786.8 nM 6.10
CHEMBL2387228 Ki = 843.6 nM 6.07
CHEMBL2387241 Ki = 987.3 nM 6.01
CHEMBL2387257 Ki = 1385.4 nM 5.86
CHEMBL2387252 Ki = 1589.6 nM 5.80
CHEMBL2387258 Ki = 1868.7 nM 5.73
CHEMBL2387244 Ki = 1928.6 nM 5.71
CHEMBL2387236 Ki = 2348.8 nM 5.63
CHEMBL2387246 Ki = 2350.3 nM 5.63
CHEMBL2387248 Ki = 2817.2 nM 5.55
CHEMBL2387267 Ki = 3012.4 nM 5.52
CHEMBL2387240 Ki > 10000.0 nM -
CHEMBL2387263 Ki > 10000.0 nM -
CHEMBL2387231 Ki > 10000.0 nM -
CHEMBL2387226 Ki > 10000.0 nM -
CHEMBL2387261 Ki > 10000.0 nM -
CHEMBL2387247 Ki > 10000.0 nM -
CHEMBL2387243 Ki > 10000.0 nM -
CHEMBL2387266 Ki > 10000.0 nM -
CHEMBL2387264 Ki > 10000.0 nM -