General Information of the Protein
Protein ID
PT02999
Protein Name
Cytochrome P450 26A1
Secondarily
Protein Name
Cytochrome P450 retinoic acid-inactivating 1
Retinoic acid 4-hydroxylase
Retinoic acid-metabolizing cytochrome
Gene Name
CYP26A1
Secondarily
Gene Name
CYP26
P450RAI1
Sequence
MGLPALLASALCTFVLPLLLFLAAIKLWDLYCVSGRDRSCALPLPPGTMGFPFFGETLQMVLQRRKFLQMKRRKYGFIYKTHLFGRPTVRVMGADNVRRILLGEHRLVSVHWPASVRTILGSGCLSNLHDSSHKQRKKVIMRAFSREALECYVPVITEEVGSSLEQWLSCGERGLLVYPEVKRLMFRIAMRILLGCEPQLAGDGDSEQQLVEAFEEMTRNLFSLPIDVPFSGLYRGMKARNLIHARIEQNIRAKICGLRASEAGQGCKDALQLLIEHSWERGERLDMQALKQSSTELLFGGHETTASAATSLITYLGLYPHVLQKVREELKSKGLLCKSNQDNKLDMEILEQLKYIGCVIKETLRLNPPVPGGFRVALKTFELNGYQIPKGWNVIYSICDTHDVAEIFTNKEEFNPDRFMLPHPEDASRFSFIPFGGGLRSCVGKEFAKILLKIFTVELARHCDWQLLNGPPTMKTSPTVYPVDNLPARFTHFHGEI
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Cytochrome P450
>
Cytochrome P450 family 26
>
Cytochrome P450 family 26A
>
Cytochrome P450 26A1
Function
A cytochrome P450 monooxygenase involved in the metabolism of retinoates (RAs), the active metabolites of vitamin A, and critical signaling molecules in animals (PubMed:22020119, PubMed:9228017, PubMed:9716180). RAs exist as at least four different isomers: all-trans-RA (atRA), 9-cis-RA, 13-cis-RA, and 9,13-dicis-RA, where atRA is considered to be the biologically active isomer, although 9-cis-RA and 13-cis-RA also have activity (Probable). Catalyzes the hydroxylation of atRA primarily at C-4 and C-18, thereby contributing to the regulation of atRA homeostasis and signaling (PubMed:22020119, PubMed:9228017, PubMed:9716180). Hydroxylation of atRA limits its biological activity and initiates a degradative process leading to its eventual elimination (Probable). Involved in the convertion of atRA to all-trans-4-oxo-RA. Able to metabolize other RAs such as 9-cis, 13-cis and 9,13-di-cis RA (By similarity) (PubMed:9228017). Can oxidize all-trans-13,14-dihydroretinoate (DRA) to metabolites which could include all-trans-4-oxo-DRA, all-trans-4-hydroxy-DRA, all-trans-5,8-epoxy-DRA, and all-trans-18-hydroxy-DRA (By similarity). May play a role in the oxidative metabolism of xenobiotics such as tazarotenic acid (PubMed:26937021).
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Uniprot ID
Primary ID:
O43174

Secondarily ID:
B3KNI4
Q5VXH9
Q5VXI0
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HGNC ID
HGNC:2603
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: CL000018 , HL-60
Compound ID Compound Name Compound Formula
CP0158477
methyl 2-[(5-chloro-3-methyl-1-phenylpyrazole-4-carbonyl)amino]-3-imidazol-1-ylpropanoate
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C18H18ClN5O3
 1
1
IC50 = 220 nM
   TI
   LI
   LO
   TS
CP0435138
methyl 3-imidazol-1-yl-2-[(4-phenylbenzoyl)amino]propanoate
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C20H19N3O3
 1
1
IC50 = 370 nM
   TI
   LI
   LO
   TS
CP0474726
methyl 2-(1,3-benzothiazole-2-carbonylamino)-3-imidazol-1-ylpropanoate
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C15H14N4O3S
 1
1
IC50 = 410 nM
   TI
   LI
   LO
   TS
CP0365786
propan-2-yl 2-[(5-chloro-3-methyl-1-phenylpyrazole-4-carbonyl)amino]-3-imidazol-1-ylpropanoate
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C20H22ClN5O3
 1
1
IC50 = 460 nM
   TI
   LI
   LO
   TS
CP0539323
propan-2-yl 3-imidazol-1-yl-2-[(4-phenylbenzoyl)amino]propanoate
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C22H23N3O3
 1
1
IC50 = 540 nM
   TI
   LI
   LO
   TS
CP0545405
ethyl 2-[(5-chloro-3-methyl-1-phenylpyrazole-4-carbonyl)amino]-3-imidazol-1-ylpropanoate
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C19H20ClN5O3
 1
1
IC50 = 600 nM
   TI
   LI
   LO
   TS
CP0555774
propyl 2-[(5-chloro-3-methyl-1-phenylpyrazole-4-carbonyl)amino]-3-imidazol-1-ylpropanoate
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C20H22ClN5O3
 1
1
IC50 = 620 nM
   TI
   LI
   LO
   TS
CP0564212
propan-2-yl 2-(1,3-benzothiazole-2-carbonylamino)-3-imidazol-1-ylpropanoate
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C17H18N4O3S
 1
1
IC50 = 630 nM
   TI
   LI
   LO
   TS
CP0422624
ethyl 3-imidazol-1-yl-2-[(4-phenylbenzoyl)amino]propanoate
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C21H21N3O3
 1
1
IC50 = 650 nM
   TI
   LI
   LO
   TS
CP0413747
ethyl 2-(1,3-benzothiazole-2-carbonylamino)-3-imidazol-1-ylpropanoate
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C16H16N4O3S
 1
1
IC50 = 740 nM
   TI
   LI
   LO
   TS
CP0438257
propyl 3-imidazol-1-yl-2-[(4-phenylbenzoyl)amino]propanoate
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C22H23N3O3
 1
1
IC50 = 790 nM
   TI
   LI
   LO
   TS
CP0564211
propyl 2-(1,3-benzothiazole-2-carbonylamino)-3-imidazol-1-ylpropanoate
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C17H18N4O3S
 1
1
IC50 = 840 nM
   TI
   LI
   LO
   TS
CP0074319
5-[(3-Chloro-phenyl)-imidazol-1-yl-methyl]-1H-benzoimidazole
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C17H13ClN4
 2
1
IC50 = 890 nM
   TI
   LI
   LO
   TS
2
IC50 = 2450 nM
   TI
   LI
   LO
   TS
CP0474724
2-methylpropyl 3-imidazol-1-yl-2-[(4-phenylbenzoyl)amino]propanoate
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C23H25N3O3
 1
1
IC50 = 970 nM
   TI
   LI
   LO
   TS
CP0539324
2-methylpropyl 2-[(5-chloro-3-methyl-1-phenylpyrazole-4-carbonyl)amino]-3-imidazol-1-ylpropanoate
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C21H24ClN5O3
 1
1
IC50 = 1020 nM
   TI
   LI
   LO
   TS
CP0444554
2-methylpropyl 2-(1,3-benzothiazole-2-carbonylamino)-3-imidazol-1-ylpropanoate
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C18H20N4O3S
 1
1
IC50 = 1110 nM
   TI
   LI
   LO
   TS
CP0494404
3-(2-bromophenyl)-3-[(5-chloro-3-methyl-1-phenylpyrazole-4-carbonyl)amino]propanoic acid
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C20H17BrClN3O3
 1
1
IC50 = 1360 nM
   TI
   LI
   LO
   TS
CP0444969
3-(3-bromophenyl)-3-[(5-chloro-3-methyl-1-phenylpyrazole-4-carbonyl)amino]propanoic acid
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C20H17BrClN3O3
 1
1
IC50 = 1870 nM
   TI
   LI
   LO
   TS
CP0429389
3-[(5-chloro-3-methyl-1-phenylpyrazole-4-carbonyl)amino]-3-(3,4-dichlorophenyl)propanoic acid
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C20H16Cl3N3O3
 1
1
IC50 = 2070 nM
   TI
   LI
   LO
   TS
CP0539938
3-(2-bromophenyl)-3-[(2,5-dimethylfuran-3-carbonyl)amino]propanoic acid
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C16H16BrNO4
 1
1
IC50 = 2340 nM
   TI
   LI
   LO
   TS
CP0456345
3-[(5-tert-butyl-2-methylfuran-3-carbonyl)amino]-3-(3,4-dichlorophenyl)propanoic acid
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C19H21Cl2NO4
 1
1
IC50 = 2620 nM
   TI
   LI
   LO
   TS
CP0444971
3-(4-chlorophenyl)-3-[(2,5-dimethylfuran-3-carbonyl)amino]propanoic acid
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C16H16ClNO4
 1
1
IC50 = 2730 nM
   TI
   LI
   LO
   TS
CP0379477
3-[(5-tert-butyl-2-methylfuran-3-carbonyl)amino]-3-(3-fluorophenyl)propanoic acid
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C19H22FNO4
 1
1
IC50 = 2810 nM
   TI
   LI
   LO
   TS
CP0399591
3-(3,4-dichlorophenyl)-3-[(2,5-dimethylfuran-3-carbonyl)amino]propanoic acid
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C16H15Cl2NO4
 1
1
IC50 = 2830 nM
   TI
   LI
   LO
   TS
CP0399592
3-[(5-tert-butyl-2-methylfuran-3-carbonyl)amino]-3-(4-chlorophenyl)propanoic acid
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C19H22ClNO4
 1
1
IC50 = 3020 nM
   TI
   LI
   LO
   TS
CP0557945
3-[(5-tert-butyl-2-methylfuran-3-carbonyl)amino]-3-(3-nitrophenyl)propanoic acid
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C19H22N2O6
 1
1
IC50 = 3040 nM
   TI
   LI
   LO
   TS
CP0557944
3-[(2,5-dimethylfuran-3-carbonyl)amino]-3-(4-methylphenyl)propanoic acid
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C17H19NO4
 1
1
IC50 = 3090 nM
   TI
   LI
   LO
   TS
CP0483369
3-(2-bromophenyl)-3-[(5-tert-butyl-2-methyl-1-propylpyrrole-3-carbonyl)amino]propanoic acid
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C22H29BrN2O3
 1
1
IC50 = 3130 nM
   TI
   LI
   LO
   TS
CP0379476
3-[(2,5-dimethylfuran-3-carbonyl)amino]-3-(3-methylphenyl)propanoic acid
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C17H19NO4
 1
1
IC50 = 3140 nM
   TI
   LI
   LO
   TS
CP0456343
3-[(5-tert-butyl-2-methylfuran-3-carbonyl)amino]-3-phenylpropanoic acid
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C19H23NO4
 1
1
IC50 = 3210 nM
   TI
   LI
   LO
   TS
CP0487798
3-(4-tert-butylphenyl)-3-[(5-chloro-3-methyl-1-phenylpyrazole-4-carbonyl)amino]propanoic acid
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C24H26ClN3O3
 1
1
IC50 = 3220 nM
   TI
   LI
   LO
   TS
CP0433435
3-[(5-tert-butyl-2-methylfuran-3-carbonyl)amino]-3-(4-methylphenyl)propanoic acid
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C20H25NO4
 1
1
IC50 = 3260 nM
   TI
   LI
   LO
   TS
CP0420212
3-[(5-tert-butyl-2-methyl-1-propylpyrrole-3-carbonyl)amino]-3-(2-nitrophenyl)propanoic acid
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C22H29N3O5
 1
1
IC50 = 3350 nM
   TI
   LI
   LO
   TS
CP0494403
3-[(5-tert-butyl-2-methyl-1-propylpyrrole-3-carbonyl)amino]-3-(4-methoxyphenyl)propanoic acid
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C23H32N2O4
 1
1
IC50 = 3480 nM
   TI
   LI
   LO
   TS
CP0498075
3-[(2,5-dimethylfuran-3-carbonyl)amino]-3-(4-propan-2-ylphenyl)propanoic acid
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C19H23NO4
 1
1
IC50 = 4020 nM
   TI
   LI
   LO
   TS
CP0444972
3-[(5-tert-butyl-2-methylfuran-3-carbonyl)amino]-3-(4-propan-2-ylphenyl)propanoic acid
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C22H29NO4
 1
1
IC50 = 5070 nM
   TI
   LI
   LO
   TS
CP0561042
3-[(5-tert-butyl-2-methyl-1-propylpyrrole-3-carbonyl)amino]-3-(4-tert-butylphenyl)propanoic acid
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C26H38N2O3
 1
1
IC50 = 5190 nM
   TI
   LI
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   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0361203
N-[4-[(1R)-2-ethyl-1-(1,2,4-triazol-1-yl)butyl]phenyl]-1,3-benzothiazol-2-amine
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C21H23N5S
 1
1 IC50 = 4 nM
CP0345809
N-[4-[imidazol-1-yl(phenyl)methyl]phenyl]naphthalen-2-amine
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C26H21N3
 1
1 IC50 = 500 nM
CP0074319
5-[(3-Chloro-phenyl)-imidazol-1-yl-methyl]-1H-benzoimidazole
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C17H13ClN4
 2
1 IC50 = 540 nM
2 IC50 = 6000 nM
Clinical Information about the Protein
Target 1 ( Cytochrome P450 26 (CYP26A1) )
Target Type Clinical trial Target
Disease 2 Target-related Diseases  2
1 Dermatological disease [ICD-11: DA24.Y]
2 Psoriasis vulgaris [ICD-11: EA90]
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 LIAROZOLE Phase 2/3
Dermatological disease
2 Rambazole Phase 2
Psoriasis vulgaris