General Information of the Protein
Protein ID
PT01002
Protein Name
Cytochrome P450 1A2
Secondarily
Protein Name
CYPIA2
Cholesterol 25-hydroxylase
Cytochrome P(3)450
Cytochrome P450 4
Cytochrome P450-P3
Hydroperoxy icosatetraenoate dehydratase
Gene Name
CYP1A2
Sequence
MALSQSVPFSATELLLASAIFCLVFWVLKGLRPRVPKGLKSPPEPWGWPLLGHVLTLGKNPHLALSRMSQRYGDVLQIRIGSTPVLVLSRLDTIRQALVRQGDDFKGRPDLYTSTLITDGQSLTFSTDSGPVWAARRRLAQNALNTFSIASDPASSSSCYLEEHVSKEAKALISRLQELMAGPGHFDPYNQVVVSVANVIGAMCFGQHFPESSDEMLSLVKNTHEFVETASSGNPLDFFPILRYLPNPALQRFKAFNQRFLWFLQKTVQEHYQDFDKNSVRDITGALFKHSKKGPRASGNLIPQEKIVNLVNDIFGAGFDTVTTAISWSLMYLVTKPEIQRKIQKELDTVIGRERRPRLSDRPQLPYLEAFILETFRHSSFLPFTIPHSTTRDTTLNGFYIPKKCCVFVNQWQVNHDPELWEDPSEFRPERFLTADGTAINKPLSEKMMLFGMGKRRCIGEVLAKWEIFLFLAILLQQLEFSVPPGVKVDLTPIYGLTMKHARCEHVQARLRFSIN
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Cytochrome P450
>
Cytochrome P450 family 1
>
Cytochrome P450 family 1A
>
Cytochrome P450 1A2
Function
A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:9435160, PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:9435160, PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:11555828, PubMed:12865317). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2 (PubMed:11555828, PubMed:12865317). Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). May act as a major enzyme for all-trans retinoic acid biosynthesis in the liver. Catalyzes two successive oxidative transformation of all-trans retinol to all-trans retinal and then to the active form all-trans retinoic acid (PubMed:10681376). Primarily catalyzes stereoselective epoxidation of the last double bond of polyunsaturated fatty acids (PUFA), displaying a strong preference for the (R,S) stereoisomer (PubMed:19965576). Catalyzes bisallylic hydroxylation and omega-1 hydroxylation of PUFA (PubMed:9435160). May also participate in eicosanoids metabolism by converting hydroperoxide species into oxo metabolites (lipoxygenase-like reaction, NADPH-independent) (PubMed:21068195). Plays a role in the oxidative metabolism of xenobiotics. Catalyzes the N-hydroxylation of heterocyclic amines and the O-deethylation of phenacetin (PubMed:14725854). Metabolizes caffeine via N3-demethylation (Probable).
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Uniprot ID
Primary ID:
P05177

Secondarily ID:
Q16754
Q6NWU3
Q6NWU5
Q9BXX7
Q9UK49
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Ensembl ID
ENSG00000140505
HGNC ID
HGNC:2596
Subcellular Location
Endoplasmic reticulum membrane
Microsome membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000023 , BTI-Tn-5B1-4
Compound ID Compound Name Compound Formula
CP0011964
10H-Phenothiazin
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C12H9NS
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0037728
5,6-dihydrophenanthridin-6-one
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C13H9NO
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0675003
N-acetyl-2-aminofluorene
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C15H13NO
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0048520
6-hydroxy-7-methoxy-5-benzofuranacrylic acid delta-lactone
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C12H8O4
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0085428
(B(a)P)
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C20H12
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0666225
Benzo(e)pyrene
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C20H12
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0039119
(4-amino-1-methyl-butyl)-(6-methoxy-8-quinolyl)amine;phosphoric acid
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C15H21N3O
 1
1
IC50 = 182.4 nM
   TI
   LI
   LO
   TS
CP0069750
1-Benzylimidazole (BI)
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C10H10N2
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0046619
Adalat
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C17H18N2O6
 1
1
IC50 = 300 nM
   TI
   LI
   LO
   TS
CP0057530
ECONAZOLE
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C18H15Cl3N2O
 1
1
IC50 = 300 nM
   TI
   LI
   LO
   TS
CP0065937
US9138393, Methyl- cholanthrene
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C21H16
 1
1
IC50 = 300 nM
   TI
   LI
   LO
   TS
CP0077040
4-Amino-5-chloro-2-ethoxy-N-[4-(4-fluoro-benzyl)-morpholin-2-ylmethyl]-benzamide; citrate(AS-4370)
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C21H25ClFN3O3
 1
1
IC50 = 400 nM
   TI
   LI
   LO
   TS
CP0041328
5-Methyl-N-(4-(trifluoromethyl)phenyl)-4-isoxazolecarboxamide
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C12H9F3N2O2
 1
1
IC50 = 500 nM
   TI
   LI
   LO
   TS
CP0072682
Exelderm
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C18H15Cl3N2S
 1
1
IC50 = 600 nM
   TI
   LI
   LO
   TS
CP0071568
5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrid[4,3-b]indol-1-one;hydrochloride
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C17H18N4O
 1
1
IC50 = 604.7 nM
   TI
   LI
   LO
   TS
CP0070572
4-(1H-benzimidazol-2-yl)-1,3-thiazole
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C10H7N3S
 1
1
IC50 = 800 nM
   TI
   LI
   LO
   TS
CP0094999
BW-723C86
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C16H18N2OS
 1
1
IC50 = 873.8 nM
   TI
   LI
   LO
   TS
CP0070921
MLS001335996
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C76H52O46
 1
1
IC50 = 919 nM
   TI
   LI
   LO
   TS
CP0038890
2-PHENYL-4H-BENZO[H]CHROMEN-4-ONE
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C19H12O2
 1
1
IC50 = 990.9 nM
   TI
   LI
   LO
   TS
CP0002420
2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
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C19H17NO3
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0042169
CHEBI:35847
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C14H9ClN2O3S
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0046649
1-Naphthyl Isothiocyanate
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C11H7NS
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0072914
US20230414632, Compound I-e
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C20H24N2O6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0048396
HEXACHLOROPHENE
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C13H6Cl6O2
 1
1
IC50 = 1313.3 nM
   TI
   LI
   LO
   TS
CP0000254
(Z)-2-(3-(4-(methylthio)benzylidene)-6-fluoro-2-methyl-3H-inden-1-yl)acetic acid
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C20H17FO2S
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0016295
4-[4-(4-fluorophenyl)-2-(4-methanesulfinylphenyl)-1H-imidazol-5-yl]pyridine
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C21H16FN3OS
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0053630
2-chloranyl-10-[3-(4-methylpiperazin-1-yl)propyl]phenothiazine;ethane-1,2-disulfonic acid
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C20H24ClN3S
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0069855
Artemisinin, 18
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C15H22O5
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0072749
3,5-Dibromo-N-(4-bromophenyl)-2-hydroxybenzamide (31)
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C13H8Br3NO2
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0084142
BS-749
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C8H9NO2
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0041805
(E)-resveratrol
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C14H12O3
 1
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0049976
(6E)-N-[(4-hydroxy-3-methoxyphenyl)methyl]-8-methylnon-6-enamide
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C18H27NO3
 1
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0011846
1-(2-(2-hydroxy-3-(propylamino)propoxy)phenyl)-3-phenylpropan-1-one
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C21H27NO3
 1
1
IC50 = 3292 nM
   TI
   LI
   LO
   TS
CP0037451
1,1',1'',1'''-[disulfanediylbis(carbonothioylnitrilo)]tetraethane
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C10H20N2S4
 1
1
IC50 = 4000 nM
   TI
   LI
   LO
   TS
CP0041613
Anapriline
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C16H21NO2
 1
1
IC50 = 4000 nM
   TI
   LI
   LO
   TS
CP0072314
ALTRETAMINE
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C9H18N6
 1
1
IC50 = 4000 nM
   TI
   LI
   LO
   TS
CP0041290
MLS000069541
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C15H16O2
 1
1
IC50 = 5000 nM
   TI
   LI
   LO
   TS
CP0082578
CHEBI:27924
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C6H8N2
 1
1
IC50 = 8000 nM
   TI
   LI
   LO
   TS
CP0035893
(Thioridazine)10-[2-(1-Methyl-piperidin-2-yl)-ethyl]-2-methylsulfanyl-10H-phenothiazine
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C21H26N2S2
 1
1
IC50 = 9332.3 nM
   TI
   LI
   LO
   TS
CP0669095
Safrole
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C10H10O2
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0038890
2-PHENYL-4H-BENZO[H]CHROMEN-4-ONE
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C19H12O2
 10
1 IC50 = 3.8 nM
2 IC50 = 6 nM
3 IC50 = 12 nM
4 IC50 = 18 nM
5 IC50 = 19 nM
6 IC50 = 49 nM
7 IC50 = 68.4 nM
8 IC50 = 32000 nM
9 IC50 = 32600 nM
10 IC50 < 1000 nM
CP0020849
2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chromen-4-one
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C15H10O7
 1
1 IC50 = 4097 nM
CP0071568
5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrid[4,3-b]indol-1-one;hydrochloride
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C17H18N4O
 1
1 IC50 < 10000 nM
CP0041613
Anapriline
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C16H21NO2
 1
1 IC50 > 10000 nM