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Assay Detail

CHEMBL4149803

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

ADMET
Inhibition of recombinant human CYP2D6 expressed in insect cell microsomes using AMMC as substrate pretreated for 30 mins followed by NADPH addition measured after 45 mins by fluorescence assay
22
Total Activities
22
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

Discovery of N-Alkyl Piperazine Side Chain Based CXCR4 Antagonists with Improved Drug-like Properties.
Tahirovic YA, Truax VM, Wilson RJ, Jecs E, Nguyen HH, Miller EJ, Kim MB, Kuo KM, Wang T, Sum CS, Cvijic ME, Schroeder GM, Wilson LJ, Liotta DC.
ACS Med Chem Lett (2018) 9 : 446 -451
PubMed 29795757 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.82 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4163611 1 7.52
CHEMBL4174290 1 6.96
CHEMBL3091687 1 6.50
CHEMBL4164702 1 5.98
CHEMBL4170857 1 5.85
CHEMBL4159150 1 5.84
CHEMBL518924 MAVORIXAFOR 4.0 1 5.79
CHEMBL4159410 1 5.73
CHEMBL4167058 1 5.67
CHEMBL4172802 1 5.53
CHEMBL4160551 1 5.38
CHEMBL4166456 1 5.38
CHEMBL4170141 1 5.29
CHEMBL4165032 1 5.25
CHEMBL4167654 1 5.22
CHEMBL4159991 1 5.18
CHEMBL4162125 1 -
CHEMBL4161613 1 -
CHEMBL4172234 1 -
CHEMBL4175653 1 -
CHEMBL4167467 1 -
CHEMBL4175350 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4163611 IC50 = 30.0 nM 7.52
CHEMBL4174290 IC50 = 110.0 nM 6.96
CHEMBL3091687 IC50 = 320.0 nM 6.50
CHEMBL4164702 IC50 = 1040.0 nM 5.98
CHEMBL4170857 IC50 = 1400.0 nM 5.85
CHEMBL4159150 IC50 = 1430.0 nM 5.84
CHEMBL518924 MAVORIXAFOR IC50 = 1640.0 nM 5.79
CHEMBL4159410 IC50 = 1870.0 nM 5.73
CHEMBL4167058 IC50 = 2140.0 nM 5.67
CHEMBL4172802 IC50 = 2960.0 nM 5.53
CHEMBL4160551 IC50 = 4140.0 nM 5.38
CHEMBL4166456 IC50 = 4210.0 nM 5.38
CHEMBL4170141 IC50 = 5140.0 nM 5.29
CHEMBL4165032 IC50 = 5600.0 nM 5.25
CHEMBL4167654 IC50 = 6040.0 nM 5.22
CHEMBL4159991 IC50 = 6650.0 nM 5.18
CHEMBL4162125 IC50 > 20000.0 nM -
CHEMBL4161613 IC50 > 20000.0 nM -
CHEMBL4172234 IC50 > 20000.0 nM -
CHEMBL4175653 IC50 > 20000.0 nM -
CHEMBL4167467 IC50 > 20000.0 nM -
CHEMBL4175350 IC50 > 20000.0 nM -