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CYP2C8

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Target not currently curated in GtoImmuPdb

Target id: 1325

Nomenclature: CYP2C8

Family: CYP2 family: drug metabolising subset

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 490 10q23.33 CYP2C8 cytochrome P450 family 2 subfamily C member 8
Previous and Unofficial Names Click here for help
cytochrome P450, subfamily IIC (mephenytoin 4-hydroxylase), polypeptide 8 | cytochrome P450, family 2, subfamily C, polypeptide 8
Database Links Click here for help
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
Pharos
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 1.14.14.1

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
phenelzine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 5.1 pKi 2
pKi 5.1 (Ki 7.266x10-6 M) [2]
compound 51 [Crosignani et al., 2011] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pIC50 1
pIC50 7.4 (IC50 4.3x10-8 M) [1]
voxelotor Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 5.1 pIC50 3
pIC50 5.1 (IC50 7.9x10-6 M) [3]
Description: Measuring inhibition of CYP2C8 activity using paclitaxel as substrate.

References

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1. Crosignani S, Jorand-Lebrun C, Campbell G, Prêtre A, Grippi-Vallotton T, Quattropani A, Bouscary-Desforges G, Bombrun A, Missotten M, Humbert Y et al.. (2011) Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids. ACS Med Chem Lett, 2 (12): 938-42. [PMID:24900284]

2. Fontana E, Dansette PM, Poli SM. (2005) Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. Curr Drug Metab, 6 (5): 413-54. [PMID:16248836]

3. Metcalf B, Chuang C, Dufu K, Patel MP, Silva-Garcia A, Johnson C, Lu Q, Partridge JR, Patskovska L, Patskovsky Y et al.. (2017) Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin. ACS Med Chem Lett, 8 (3): 321-326. [PMID:28337324]

Contributors

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