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Assay Detail

CHEMBL4709840

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

Binding
Displacement of [3H]spiperone from D2 receptor in rat striatum measured after 15 mins by liquid scintillation counting method
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Isoquinolinone derivatives as potent CNS multi-receptor D/5-HT/5-HT/5-HT/5-HT agents: Synthesis and pharmacological evaluation.
Jin J,Zhang K,Dou F,Hao C,Zhang Y,Cao X,Gao L,Xiong J,Liu X,Liu BF,Zhang G,Chen Y
Eur J Med Chem (2020) 207 : 112709 -112709
PubMed 32877805 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 6.79 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 8.43
CHEMBL4764679 1 8.16
CHEMBL4743324 1 8.04
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.01
CHEMBL3965773 1 7.53
CHEMBL4783375 1 7.38
CHEMBL4749019 1 7.17
CHEMBL4777373 1 6.93
CHEMBL4779075 1 6.91
CHEMBL3911283 1 6.79
CHEMBL4746373 1 6.60
CHEMBL4781390 1 6.58
CHEMBL4749033 1 6.57
CHEMBL4759887 1 6.50
CHEMBL4790565 1 6.45
CHEMBL4753384 1 6.41
CHEMBL4778204 1 6.27
CHEMBL4742251 1 6.25
CHEMBL4797306 1 6.16
CHEMBL4788000 1 6.05
CHEMBL4741087 1 6.04
CHEMBL4754923 1 6.04
CHEMBL4795213 1 5.91
CHEMBL4761213 1 5.86
CHEMBL4758213 1 -
CHEMBL4761618 1 -
CHEMBL4800484 1 -
CHEMBL4798115 1 -
CHEMBL4756417 1 -
CHEMBL4795287 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 3.7 nM 8.43
CHEMBL4764679 Ki = 6.9 nM 8.16
CHEMBL4743324 Ki = 9.2 nM 8.04
CHEMBL1112 ARIPIPRAZOLE Ki = 9.7 nM 8.01
CHEMBL3965773 Ki = 29.3 nM 7.53
CHEMBL4783375 Ki = 41.6 nM 7.38
CHEMBL4749019 Ki = 68.2 nM 7.17
CHEMBL4777373 Ki = 117.2 nM 6.93
CHEMBL4779075 Ki = 123.2 nM 6.91
CHEMBL3911283 Ki = 161.9 nM 6.79
CHEMBL4746373 Ki = 249.2 nM 6.60
CHEMBL4781390 Ki = 261.4 nM 6.58
CHEMBL4749033 Ki = 268.3 nM 6.57
CHEMBL4759887 Ki = 316.3 nM 6.50
CHEMBL4790565 Ki = 359.2 nM 6.45
CHEMBL4753384 Ki = 391.2 nM 6.41
CHEMBL4778204 Ki = 532.4 nM 6.27
CHEMBL4742251 Ki = 568.2 nM 6.25
CHEMBL4797306 Ki = 698.0 nM 6.16
CHEMBL4788000 Ki = 896.0 nM 6.05
CHEMBL4741087 Ki = 923.0 nM 6.04
CHEMBL4754923 Ki = 902.0 nM 6.04
CHEMBL4795213 Ki = 1237.0 nM 5.91
CHEMBL4761213 Ki = 1368.0 nM 5.86
CHEMBL4758213 Ki > 10000.0 nM -
CHEMBL4761618 Ki > 10000.0 nM -
CHEMBL4800484 Ki > 10000.0 nM -
CHEMBL4798115 Ki > 10000.0 nM -
CHEMBL4756417 Ki > 10000.0 nM -
CHEMBL4795287 Ki > 10000.0 nM -
CHEMBL4751120 Ki > 10000.0 nM -
CHEMBL4743127 Ki > 10000.0 nM -