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Assay Detail

CHEMBL5048796

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

ADMET
Inhibition of recombinant human CYP2D6 using AMMC as substrate preincubated for 30 mins followed by substrate addition measured after 45 mins by fluorescence based assay
25
Total Activities
25
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

Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles.
Jecs E, Tahirovic YA, Wilson RJ, Miller EJ, Kim M, Truax V, Nguyen HH, Akins NS, Saindane M, Wang T, Sum CS, Cvijic ME, Schroeder GM, Burton SL, Derdeyn CA, Xu L, Jiang Y, Wilson LJ, Liotta DC.
J Med Chem (2022) 65 : 4058 -4084
PubMed 35179893 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.23 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3091687 1 6.50
CHEMBL5070403 1 6.16
CHEMBL5087754 1 5.57
CHEMBL5085636 1 5.57
CHEMBL5079518 1 5.55
CHEMBL5076569 1 5.40
CHEMBL5079671 1 5.36
CHEMBL5086715 1 5.01
CHEMBL5080863 1 5.00
CHEMBL5082441 1 5.00
CHEMBL5070958 1 4.92
CHEMBL5093818 1 4.89
CHEMBL5092098 1 4.89
CHEMBL5079186 1 4.89
CHEMBL5078032 1 4.82
CHEMBL5091696 1 4.75
CHEMBL5078984 1 4.70
CHEMBL5084366 1 -
CHEMBL5083811 1 -
CHEMBL5085511 1 -
CHEMBL5077132 1 -
CHEMBL5083458 1 -
CHEMBL5092949 1 -
CHEMBL5081505 1 -
CHEMBL5082142 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3091687 IC50 = 320.0 nM 6.50
CHEMBL5070403 IC50 = 700.0 nM 6.16
CHEMBL5087754 IC50 = 2700.0 nM 5.57
CHEMBL5085636 IC50 = 2700.0 nM 5.57
CHEMBL5079518 IC50 = 2800.0 nM 5.55
CHEMBL5076569 IC50 = 4000.0 nM 5.40
CHEMBL5079671 IC50 = 4400.0 nM 5.36
CHEMBL5086715 IC50 = 9700.0 nM 5.01
CHEMBL5080863 IC50 = 10000.0 nM 5.00
CHEMBL5082441 IC50 = 10000.0 nM 5.00
CHEMBL5070958 IC50 = 12000.0 nM 4.92
CHEMBL5093818 IC50 = 13000.0 nM 4.89
CHEMBL5092098 IC50 = 13000.0 nM 4.89
CHEMBL5079186 IC50 = 13000.0 nM 4.89
CHEMBL5078032 IC50 = 15000.0 nM 4.82
CHEMBL5091696 IC50 = 18000.0 nM 4.75
CHEMBL5078984 IC50 = 20000.0 nM 4.70
CHEMBL5084366 IC50 > 20000.0 nM -
CHEMBL5083811 IC50 > 20000.0 nM -
CHEMBL5085511 IC50 > 20000.0 nM -
CHEMBL5077132 IC50 > 20000.0 nM -
CHEMBL5083458 IC50 > 20000.0 nM -
CHEMBL5092949 IC50 > 20000.0 nM -
CHEMBL5081505 IC50 > 20000.0 nM -
CHEMBL5082142 IC50 > 20000.0 nM -