CYP2D6

Target id: 1329

Nomenclature: CYP2D6

Family: CYP2 family

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for CYP2D6 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - CYP2D6 cytochrome P450 family 2 subfamily D member 6
Previous and Unofficial Names
Debrisoquine 4-hydroxylase | cytochrome P450, subfamily IID (debrisoquine, sparteine, etc., -metabolising), polypeptide 8 pseudogene 2 | cytochrome P450, subfamily IID (debrisoquine, sparteine, etc., -metabolizing), polypeptide 6 | cytochrome P450, subfamily 2D, polypeptide 6 | cytochrome P450, subfamily II (debrisoquine, sparteine, etc., -metabolising), polypeptide 7 pseudogene 2 | cytochrome P450, family 2, subfamily D, polypeptide 6
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
SynPHARM
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 1.14.14.1
Substrates and Reaction Kinetics
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
bufuralol N/A - - 1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
ajmalicine Hs Inhibition 8.5 pKi 3
pKi 8.5 (Ki 3.3x10-9 M) [3]
TIQ-15 Hs Inhibition 6.5 pIC50 2
pIC50 6.5 (IC50 3.2x10-7 M) [2]
compound 46c [PMID: 29350534] Hs Inhibition 5.6 pIC50 2
pIC50 5.6 (IC50 2.61x10-6 M) [2]

References

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1. Lindmark B, Lundahl A, Kanebratt KP, Andersson TB, Isin EM. (2018) Human hepatocytes and cytochrome P450-selective inhibitors predict variability in human drug exposure more accurately than human recombinant P450s. Br. J. Pharmacol., [Epub ahead of print]. [PMID:29574682]

2. Miller EJ, Jecs E, Truax VM, Katzman BM, Tahirovic YA, Wilson RJ, Kuo KM, Kim MB, Nguyen HH, Saindane MT et al.. (2018) Discovery of Tetrahydroisoquinoline-Containing CXCR4 Antagonists with Improved in Vitro ADMET Properties. J. Med. Chem., 61 (3): 946-979. [PMID:29350534]

3. Strobl GR, von Kruedener S, Stöckigt J, Guengerich FP, Wolff T. (1993) Development of a pharmacophore for inhibition of human liver cytochrome P-450 2D6: molecular modeling and inhibition studies. J. Med. Chem., 36 (9): 1136-45. [PMID:8487254]

How to cite this page

CYP2 family: CYP2D6. Last modified on 17/04/2018. Accessed on 24/05/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1329.