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Assay Detail

CHEMBL2350844

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

ADMET
Inhibition of CYP2D6 (unknown origin)
8
Total Activities
8
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

Cytochrome P450 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.
Padilla F, Bhagirath N, Chen S, Chiao E, Goldstein DM, Hermann JC, Hsu J, Kennedy-Smith JJ, Kuglstatter A, Liao C, Liu W, Lowrie LE, Luk KC, Lynch SM, Menke J, Niu L, Owens TD, O-Yang C, Railkar A, Schoenfeld RC, Slade M, Steiner S, Tan YC, Villaseñor AG, Wang C, Wanner J, Xie W, Xu D, Zhang X, Zhou M, Lucas MC.
J Med Chem (2013) 56 : 1677 -1692
PubMed 23350847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.95 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2347409 1 5.52
CHEMBL2347407 1 5.30
CHEMBL2347420 1 4.96
CHEMBL2347999 1 4.92
CHEMBL2347406 1 4.92
CHEMBL2347416 1 4.72
CHEMBL2347419 1 4.32
CHEMBL2348858 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2347409 IC50 = 3000.0 nM 5.52
CHEMBL2347407 IC50 = 5000.0 nM 5.30
CHEMBL2347420 IC50 = 11000.0 nM 4.96
CHEMBL2347999 IC50 = 12000.0 nM 4.92
CHEMBL2347406 IC50 = 12000.0 nM 4.92
CHEMBL2347416 IC50 = 19000.0 nM 4.72
CHEMBL2347419 IC50 = 48000.0 nM 4.32
CHEMBL2348858 IC50 > 8000.0 nM -