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Assay Detail

CHEMBL4670399

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

ADMET
Displacement of [3H]methylspiperone from human D2 receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by Microbeta2 scintillation counting method
34
Total Activities
34
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of Novel pERK1/2- or β-Arrestin-Preferring 5-HT Receptor-Biased Agonists: Diversified Therapeutic-like versus Side Effect Profile.
Sniecikowska J,Gluch-Lutwin M,Bucki A,Więckowska A,Siwek A,Jastrzebska-Wiesek M,Partyka A,Wilczyńska D,Pytka K,Latacz G,Przejczowska-Pomierny K,Wyska E,Wesołowska A,Pawłowski M,Newman-Tancredi A,Kolaczkowski M
J Med Chem (2020) 63 : 10946 -10971
PubMed 32883072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 6.52 7.54
pKi 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4790600 1 7.54
CHEMBL4800575 1 6.47
CHEMBL4743868 1 6.36
CHEMBL4751777 1 6.17
CHEMBL4756322 1 6.04
CHEMBL4750444 1 -
CHEMBL4746386 1 -
CHEMBL4741857 1 -
CHEMBL56 8-OH-DPAT 1 -
CHEMBL230963 1 -
CHEMBL4753394 1 -
CHEMBL4747083 1 -
CHEMBL4790662 1 -
CHEMBL4786067 1 -
CHEMBL4797752 1 -
CHEMBL4759759 1 -
CHEMBL4797282 1 -
CHEMBL4757755 1 -
CHEMBL4756233 1 -
CHEMBL4744067 1 -
CHEMBL4756041 1 -
CHEMBL4740430 1 -
CHEMBL4760621 1 -
CHEMBL4752177 1 -
CHEMBL4755058 1 -
CHEMBL4760666 1 -
CHEMBL4796345 1 -
CHEMBL4781985 1 -
CHEMBL49 BUSPIRONE 4.0 1 -
CHEMBL4777581 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4790600 Ki = 28.84 nM 7.54
CHEMBL4800575 Ki = 338.84 nM 6.47
CHEMBL4743868 Ki = 436.52 nM 6.36
CHEMBL4751777 Ki = 676.08 nM 6.17
CHEMBL4756322 Ki = 912.01 nM 6.04
CHEMBL56 8-OH-DPAT pKi - -
CHEMBL4760271 Ki > 1000.0 nM -
CHEMBL230963 Ki > 1000.0 nM -
CHEMBL4753394 Ki > 1000.0 nM -
CHEMBL4747083 Ki > 1000.0 nM -
CHEMBL4790662 Ki > 1000.0 nM -
CHEMBL4786067 Ki > 1000.0 nM -
CHEMBL4797752 Ki > 1000.0 nM -
CHEMBL4759759 Ki > 1000.0 nM -
CHEMBL4797282 Ki > 1000.0 nM -
CHEMBL4746386 Ki > 1000.0 nM -
CHEMBL4747425 Ki > 1000.0 nM -
CHEMBL4752833 Ki > 1000.0 nM -
CHEMBL4739908 Ki > 1000.0 nM -
CHEMBL4741857 Ki > 1000.0 nM -
CHEMBL4750444 Ki > 1000.0 nM -
CHEMBL4757755 Ki > 1000.0 nM -
CHEMBL4756233 Ki > 1000.0 nM -
CHEMBL4744067 Ki > 1000.0 nM -
CHEMBL4756041 Ki > 1000.0 nM -
CHEMBL4740430 Ki > 1000.0 nM -
CHEMBL4760621 Ki > 1000.0 nM -
CHEMBL4752177 Ki > 1000.0 nM -
CHEMBL4755058 Ki > 1000.0 nM -
CHEMBL4760666 Ki > 1000.0 nM -
CHEMBL4796345 Ki > 1000.0 nM -
CHEMBL4781985 Ki > 1000.0 nM -
CHEMBL49 BUSPIRONE pKi - -
CHEMBL4777581 Ki > 1000.0 nM -