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Assay Detail

CHEMBL4392174

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ADMET
Agonist activity at human D2L receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Dopamine D4 Receptor-Selective Compounds Reveal Structure-Activity Relationships that Engender Agonist Efficacy.
Keck TM, Free RB, Day MM, Brown SL, Maddaluna MS, Fountain G, Cooper C, Fallon B, Holmes M, Stang CT, Burkhardt R, Bonifazi A, Ellenberger MP, Newman AH, Sibley DR, Wu C, Boateng CA.
J Med Chem (2019) 62 : 3722 -3740
PubMed 30883109 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 6.24 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4464861 1 7.30
CHEMBL4454068 1 6.81
CHEMBL4448320 1 6.12
CHEMBL4442548 1 5.80
CHEMBL4592753 1 5.71
CHEMBL4443054 1 5.68
CHEMBL216393 1 -
CHEMBL4473792 1 -
CHEMBL4436479 1 -
CHEMBL4587925 1 -
CHEMBL4572245 1 -
CHEMBL4473652 1 -
CHEMBL4588808 1 -
CHEMBL4437912 1 -
CHEMBL4443848 1 -
CHEMBL4591118 1 -
CHEMBL4453069 1 -
CHEMBL375596 1 -
CHEMBL4456754 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4464861 EC50 = 50.1 nM 7.30
CHEMBL4454068 EC50 = 154.0 nM 6.81
CHEMBL4448320 EC50 = 763.0 nM 6.12
CHEMBL4442548 EC50 = 1600.0 nM 5.80
CHEMBL4592753 EC50 = 1965.0 nM 5.71
CHEMBL4443054 EC50 = 2092.0 nM 5.68
CHEMBL216393 EC50 - -
CHEMBL4473792 EC50 - -
CHEMBL4436479 EC50 - -
CHEMBL4587925 EC50 - -
CHEMBL4572245 EC50 - -
CHEMBL4473652 EC50 - -
CHEMBL4588808 EC50 - -
CHEMBL4437912 EC50 - -
CHEMBL4443848 EC50 - -
CHEMBL4591118 EC50 - -
CHEMBL4453069 EC50 - -
CHEMBL375596 EC50 - -
CHEMBL4456754 EC50 - -