U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Approval Year

Unknown
139594
Substance Class Protein
Created
by admin
on Sat Dec 16 05:16:59 GMT 2023
Edited
by admin
on Sat Dec 16 05:16:59 GMT 2023
Protein Type ENZYME
Protein Sub Type CYTOCHROME P450
Sequence Origin HUMAN
Sequence Type COMPLETE
Record UNII
VK4SQL11C0
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CYTOCHROME P450 1A2
Common Name English
CYTOCHROME P450-P3
Common Name English
CYP1A2
Common Name English
CYTOCHROME P(3)450
Common Name English
HUMAN CYTOCHROME P450 1A2
Common Name English
CYTOCHROME P 450 1A2
Common Name English
Code System Code Type Description
CAS
165885-24-5
Created by admin on Sat Dec 16 05:17:09 GMT 2023 , Edited by admin on Sat Dec 16 05:17:09 GMT 2023
PRIMARY
UNIPROT
P05177
Created by admin on Sat Dec 16 05:17:09 GMT 2023 , Edited by admin on Sat Dec 16 05:17:09 GMT 2023
PRIMARY
FDA UNII
VK4SQL11C0
Created by admin on Sat Dec 16 05:17:09 GMT 2023 , Edited by admin on Sat Dec 16 05:17:09 GMT 2023
PRIMARY
Related Record Type Details
Structure of TAFENOQUINE
INHIBITOR -> METABOLIC ENZYME
Ki
Structure of PIMOBENDAN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of DEFERASIROX
SUBSTRATE -> METABOLIC ENZYME
Structure of SULFORAPHANE
INHIBITOR -> METABOLIC ENZYME
Inhibits both CYP2E1 and CYP1A2-mediated genotoxicity therefore is relevant to human isoforms of these enzymes and may contribute to a chemopreventative activity of brocolli and related species.
Structure of ALOSETRON
SUBSTRATE -> METABOLIC ENZYME
Alosetron is metabolized by human microsomal cytochrome P450 (CYP), shown in vitro to involve enzymes 2C9 (30%), 3A4 (18%), and 1A2 (10%).
MAJOR
Structure of OLANZAPINE
SUBSTRATE -> METABOLIC ENZYME
Structure of GDC-0425
SUBSTRATE -> METABOLIC ENZYME
Structure of RUCAPARIB
INHIBITOR -> METABOLIC ENZYME
REVERSIBLE
Structure of STIRIPENTOL
INHIBITOR -> METABOLIC ENZYME
Structure of ACETAMINOPHEN
SUBSTRATE -> METABOLIC ENZYME
Structure of ALVESPIMYCIN
SUBSTRATE -> METABOLIC ENZYME
Structure of EAPB-0503
SUBSTRATE -> METABOLIC ENZYME
Structure of Belumosudil
INHIBITOR -> METABOLIC ENZYME
Inhibits at clinically relevant concentrations.
Structure of TERIFLUNOMIDE
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of EXEMESTANE
SUBSTRATE -> METABOLIC ENZYME
Structure of VILOXAZINE
INHIBITOR -> METABOLIC ENZYME
REVERSIBLE
CYTOCHROME P450 1A2 (CANINE)
ANIMAL ORTHOLOG->HUMAN ORTHOLOG
Structure of TRILACICLIB
INDUCER -> METABOLIC ENZYME
Structure of 2,3,7-TRICHLORODIBENZO-P-DIOXIN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of Desloratadine
NON-INHIBITOR -> METABOLIC ENZYME
Structure of DIPHENHYDRAMINE
SUBSTRATE -> METABOLIC ENZYME
CYP1A2, CYP2C9, and CYP2C19 are involved in the metabolism of diphenhydramine as low-affinity P450 isozymes.
Structure of LONAFARNIB
SUBSTRATE -> METABOLIC ENZYME
IN VITRO
Structure of MKC-963
SUBSTRATE -> METABOLIC ENZYME
Structure of CHLORPYRIFOS
INHIBITOR -> METABOLIC ENZYME
Chlorpyrifos inhibited CYP1A1/2 activities more than 90%.
Structure of ETHINYL ESTRADIOL
SUBSTRATE -> METABOLIC ENZYME
Structure of OSU-6162
SUBSTRATE -> METABOLIC ENZYME
Structure of ZIMLOVISERTIB
NON-INHIBITOR -> METABOLIC ENZYME
Structure of NAPROXEN
SUBSTRATE -> METABOLIC ENZYME
Structure of OBETICHOLIC ACID
INHIBITOR OF EXPRESSION->METABOLIC ENZYME
The effect of 10 mg OCA on CYP1A2 substrate caffeine showed that systemicexposure to caffeine increased by 42%. The systemic exposure to caffeine increased by 65% following 25 mg OCA.
Structure of OSILODROSTAT
INHIBITOR -> METABOLIC ENZYME
MODERATE INHIBITION
Structure of THEOPHYLLINE
SUBSTRATE -> METABOLIC ENZYME
Structure of C-1311
INHIBITOR -> METABOLIC ENZYME
time- and concentration-dependent inhibitor
Structure of PIRFENIDONE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of MDMC
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of EDARAVONE
INDUCER -> METABOLIC ENZYME
Edaravone inhib it e d CYP2C9, BCRP, OAT3, and induced CYP1A2 in vitro.
Structure of SARIZOTAN
SUBSTRATE -> METABOLIC ENZYME
Structure of GNE-0877
INHIBITOR -> METABOLIC ENZYME
Structure of ROFECOXIB
SUBSTRATE -> METABOLIC ENZYME
Structure of ZILEUTON
SUBSTRATE -> METABOLIC ENZYME
Structure of Tuspetinib
SUBSTRATE -> METABOLIC ENZYME
Structure of LANSOPRAZOLE
INDUCER -> METABOLIC ENZYME
Structure of C-1330
INHIBITOR -> METABOLIC ENZYME
Structure of LUMATEPERONE
SUBSTRATE -> METABOLIC ENZYME
Structure of CRISABOROLE
SUBSTRATE -> METABOLIC ENZYME
Structure of LORCASERIN
SUBSTRATE -> METABOLIC ENZYME
Structure of ROPIVACAINE
SUBSTRATE -> METABOLIC ENZYME
Structure of TACRINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of NAPHTHALENE
SUBSTRATE -> METABOLIC ENZYME
Structure of TEGASEROD
INHIBITOR -> METABOLIC ENZYME
Ki
Structure of 3-ISOXAZOLECARBOXAMIDE, N-(2,4-DICHLOROPHENYL)-5-METHYL-
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of CIMETIDINE
INHIBITOR -> METABOLIC ENZYME
POTENT
Structure of TRICLABENDAZOLE SULFOXIDE
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of DEUTETRABENAZINE
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of 2-AMINO-1-METHYL-6-PHENYLIMIDAZO(4,5-B)PYRIDINE
SUBSTRATE -> METABOLIC ENZYME
Structure of WARFARIN, (R)-
SUBSTRATE -> METABOLIC ENZYME
Structure of DRONABINOL
INHIBITOR -> METABOLIC ENZYME
Structure of ANAGRELIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of CINACALCET
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of LOMITAPIDE
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of SILIBININ A
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of TAPINAROF
SUBSTRATE -> METABOLIC ENZYME
EC50
Structure of VELIPARIB
SUBSTRATE -> METABOLIC ENZYME
Structure of TROPISETRON
SUBSTRATE -> METABOLIC ENZYME
Structure of ANETHOLTRITHION
SUBSTRATE -> METABOLIC ENZYME
Structure of ORANTINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of PIGMENT YELLOW 74
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of SULINDAC
SUBSTRATE -> METABOLIC ENZYME
Structure of ZOLPIDEM
SUBSTRATE -> METABOLIC ENZYME
Structure of ALLITINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of FLIBANSERIN
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of MALATHION
INHIBITOR -> METABOLIC ENZYME
Malathion inhibited CYP1A1/2 activities more than 90%.
Structure of PARATHION
SUBSTRATE -> METABOLIC ENZYME
Structure of JANEX-1
SUBSTRATE -> METABOLIC ENZYME
Structure of ENASIDENIB
SUBSTRATE -> METABOLIC ENZYME
Structure of CIPROFLOXACIN
INHIBITOR -> METABOLIC ENZYME
POTENT
Structure of ENZALUTAMIDE
INHIBITOR -> METABOLIC ENZYME
TIME-DEPENDENT INHIBITION
Structure of 4'-METHYL-.ALPHA.-PYRROLIDINOBUTIOPHENONE
SUBSTRATE -> METABOLIC ENZYME
HUMAN LIVER
TISSUE EXPRESSION -> PARENT
Structure of LOFEXIDINE
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of NABUMETONE
SUBSTRATE -> METABOLIC ENZYME
Structure of BRANEBRUTINIB
INHIBITOR -> METABOLIC ENZYME
Structure of TIZANIDINE
SUBSTRATE -> METABOLIC ENZYME
Structure of SONIDEGIB
NON-INDUCER -> METABOLIC ENZYME
compared to positive controls
Structure of E-NORENDOXIFEN
INHIBITOR -> METABOLIC ENZYME
E-Norendoxifen inhibited CYP1A2 2.0-fold more potently than Z-norendoxifen.
Structure of OXYMETAZOLINE
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of PF-06835919
NON-INHIBITOR -> METABOLIC ENZYME
IC50
Structure of CARVEDILOL
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of DAPSONE
SUBSTRATE -> METABOLIC ENZYME
Structure of TRICLABENDAZOLE SULFONE
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of ELTROMBOPAG
SUBSTRATE -> METABOLIC ENZYME
Structure of IMIPRAMINE
SUBSTRATE -> METABOLIC ENZYME
10%-20% OF TOTAL METABOLISM
Structure of 2,4-DICHLOROANILINE
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of ANTIPYRINE
SUBSTRATE -> METABOLIC ENZYME
Structure of APOMORPHINE
INDUCER -> METABOLIC ENZYME
MAXIMUM FOLD INCREASE
Structure of TRICLABENDAZOLE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of PRALSETINIB
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of CAFFEINE
INDUCER -> METABOLIC ENZYME
Structure of AMIODARONE
INHIBITOR -> METABOLIC ENZYME
POTENT
Structure of FEBUXOSTAT
SUBSTRATE -> METABOLIC ENZYME
Structure of RUCAPARIB
INDUCER -> METABOLIC ENZYME
Structure of DIETHYLTOLUAMIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of VERUBECESTAT
NON-INHIBITOR -> METABOLIC ENZYME
Structure of S-16020
SUBSTRATE -> METABOLIC ENZYME
Structure of CLOZAPINE
SUBSTRATE -> METABOLIC ENZYME
Structure of VERUBECESTAT
NON-INDUCER -> METABOLIC ENZYME
Structure of MIDOMAFETAMINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of NOMIFENSINE
SUBSTRATE -> METABOLIC ENZYME
Structure of FROVATRIPTAN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of PHENACETIN
SUBSTRATE -> METABOLIC ENZYME
Structure of KB-0742
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of ASENAPINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of MOMELOTINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of DAPTOMYCIN
NON-INHIBITOR -> METABOLIC ENZYME
Structure of RIFAMYCIN
INHIBITOR -> METABOLIC ENZYME
Rifamycin is an inhibitor of CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4/5 in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose clinically relevant inhibition of these enzymes in vivo is unlikely.
Structure of UAB-30
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of NE-100 FREE BASE
SUBSTRATE -> METABOLIC ENZYME
Structure of RILUZOLE
SUBSTRATE -> METABOLIC ENZYME
Structure of IXAZOMIB
SUBSTRATE -> METABOLIC ENZYME
Structure of VOXILAPREVIR
SUBSTRATE -> METABOLIC ENZYME
Structure of ETORICOXIB
SUBSTRATE -> METABOLIC ENZYME
Structure of SONIDEGIB
NON-INHIBITOR -> METABOLIC ENZYME
No time dependent inhibition upto 50 micromolar
Structure of 2-(3-FLUOROPHENYL)-5-HYDROXY-6-METHOXY-4(1H)-QUINOLINONE
INHIBITOR -> METABOLIC ENZYME
Structure of ISTRADEFYLLINE
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of PROPANAMIDE, N-(5-(2-(2-METHOXY-3-PYRIDINYL)-7-METHYLIMIDAZO(1,2-A)PYRIDIN-3-YL)-6-(2-(1-METHYL-6-ISOQUINOLINYL)ETHYNYL)-2-PYRIDINYL)-2-(METHYLAMINO)-, (2S)-
INHIBITOR -> METABOLIC ENZYME
Structure of CARBAMAZEPINE
INDUCER -> METABOLIC ENZYME
Structure of .ALPHA.-PYRROLIDINOPENTIOPHENONE
SUBSTRATE -> METABOLIC ENZYME
Structure of EAPB-0203
SUBSTRATE -> METABOLIC ENZYME
Structure of RASAGILINE
SUBSTRATE -> METABOLIC ENZYME
Structure of BORTEZOMIB
SUBSTRATE -> METABOLIC ENZYME
Structure of COBICISTAT
NON-INHIBITOR -> METABOLIC ENZYME
Structure of RAMELTEON
SUBSTRATE -> METABOLIC ENZYME
Structure of ABAMETAPIR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of RIFAMPIN
INDUCER -> METABOLIC ENZYME
POTENT
Structure of ENCORAFENIB
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of CYCLOBENZAPRINE
SUBSTRATE -> METABOLIC ENZYME
Structure of VILOXAZINE
INDUCER -> METABOLIC ENZYME
Structure of POMALIDOMIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of SELEGILINE
SUBSTRATE -> METABOLIC ENZYME
Structure of PF-06821497
NON-INHIBITOR -> METABOLIC ENZYME
Structure of GABAPENTIN ENACARBIL
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of TASIMELTEON
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of OTESECONAZOLE
NON-INHIBITOR -> METABOLIC ENZYME
Structure of TETRABENAZINE
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of MDE
MDE
SUBSTRATE -> METABOLIC ENZYME
Structure of GNE-0877
INDUCER -> METABOLIC ENZYME
Structure of ALVAMELINE
SUBSTRATE -> METABOLIC ENZYME
Structure of PHENTHOATE
INHIBITOR -> METABOLIC ENZYME
Phenthoate inhibited CYP1A1/2 activities more than 90%.
Structure of METHOXYCHLOR
SUBSTRATE -> METABOLIC ENZYME
Structure of PALONOSETRON
SUBSTRATE -> METABOLIC ENZYME
Structure of CAFFEINE
SUBSTRATE -> METABOLIC ENZYME
Structure of BUTYLPHTHALIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of RUCAPARIB
SUBSTRATE -> METABOLIC ENZYME
In vitro, rucaparib was metabolized primarily by CYP2D6 and to a lesser extent by CYP1A2 and CYP3A4.
Structure of ALDUMASTAT
SUBSTRATE -> METABOLIC ENZYME
Structure of FENITROTHION
INHIBITOR -> METABOLIC ENZYME
Fenitrothion inhibited CYP1A1/2 activities more than 90%.
Structure of SELUMETINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of Binimetinib
SUBSTRATE -> METABOLIC ENZYME
Structure of DACARBAZINE
SUBSTRATE -> METABOLIC ENZYME
Structure of ATAZANAVIR
INHIBITOR -> METABOLIC ENZYME
COMPETITIVE INHIBITOR
Ki
Structure of UMBRALISIB
SUBSTRATE -> METABOLIC ENZYME
Structure of PARATHION-METHYL
SUBSTRATE -> METABOLIC ENZYME
Structure of OTESECONAZOLE
INDUCER -> METABOLIC ENZYME
mRNA levels in at least 2 hepatocyte cultures. Up 10 micromolar OTESECONAZOLE
Structure of Roflumilast
SUBSTRATE -> METABOLIC ENZYME
Structure of TRAMADOL
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of ROFECOXIB
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of NORENDOXIFEN
INHIBITOR -> METABOLIC ENZYME
E-Norendoxifen inhibited CYP1A2 2.0-fold more potently than Z-norendoxifen.
Structure of RIVOGLITAZONE
SUBSTRATE -> METABOLIC ENZYME
Structure of ORANTINIB
INDUCER -> METABOLIC ENZYME
Structure of ABIRATERONE
INHIBITOR -> METABOLIC ENZYME
In vitro studies with human hepatic microsomes showed that abiraterone has the potential to inhibit CYP1A2, CYP2D6, CYP2C8 and to a lesser extent CYP2C9, CYP2C19 and CYP3A4/5.
Structure of PRACINOSTAT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of OMEPRAZOLE
INDUCER -> METABOLIC ENZYME
Structure of APREPITANT
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of TRICLABENDAZOLE
INHIBITOR -> METABOLIC ENZYME
Structure of DULOXETINE
SUBSTRATE -> METABOLIC ENZYME
Structure of PROFENOFOS
INHIBITOR -> METABOLIC ENZYME
Profenofos inhibited CYP1A1/2 activities more than 90%.
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL
Molecular Formula CHEMICAL
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