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Assay Detail

CHEMBL4392168

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ADMET
Displacement of [3H](R)-(+)-7-OH-DPAT from human D2L receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293
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
Ki 11 6.35 7.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4464861 1 7.09
CHEMBL216393 1 6.90
CHEMBL4473652 1 6.70
CHEMBL4454068 1 6.70
CHEMBL375596 1 6.60
CHEMBL4442548 1 6.22
CHEMBL4588808 1 5.83
CHEMBL4443054 1 5.62
CHEMBL4448320 1 5.48
CHEMBL4587925 1 -
CHEMBL4572245 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4464861 Ki = 80.3 nM 7.09
CHEMBL216393 Ki = 127.0 nM 6.90
CHEMBL4473652 Ki = 200.0 nM 6.70
CHEMBL4454068 Ki = 200.0 nM 6.70
CHEMBL375596 Ki = 251.0 nM 6.60
CHEMBL4442548 Ki = 603.0 nM 6.22
CHEMBL4588808 Ki = 1490.0 nM 5.83
CHEMBL4443054 Ki = 2420.0 nM 5.62
CHEMBL4448320 Ki = 3320.0 nM 5.48
CHEMBL4587925 Ki > 10000.0 nM -
CHEMBL4572245 Ki > 10000.0 nM -