General Information of the Protein
Protein ID
PT02724
Protein Name
Kynurenine 3-monooxygenase
Secondarily
Protein Name
Kynurenine 3-hydroxylase
Gene Name
KMO
Sequence
MDSSVIQRKKVAVIGGGLVGSLQACFLAKRNFQIDVYEAREDTRVATFTRGRSINLALSHRGRQALKAVGLEDQIVSQGIPMRARMIHSLSGKKSAIPYGTKSQYILSVSRENLNKDLLTAAEKYPNVKMHFNHRLLKCNPEEGMITVLGSDKVPKDVTCDLIVGCDGAYSTVRSHLMKKPRFDYSQQYIPHGYMELTIPPKNGDYAMEPNYLHIWPRNTFMMIALPNMNKSFTCTLFMPFEEFEKLLTSNDVVDFFQKYFPDAIPLIGEKLLVQDFFLLPAQPMISVKCSSFHFKSHCVLLGDAAHAIVPFFGQGMNAGFEDCLVFDELMDKFSNDLSLCLPVFSRLRIPDDHAISDLSMYNYIEMRAHVNSSWFIFQKNMERFLHAIMPSTFIPLYTMVTFSRIRYHEAVQRWHWQKKVINKGLFFLGSLIAISSTYLLIHYMSPRSFLRLRRPWNWIAHFRNTTCFPAKAVDSLEQISNLISR
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Oxidoreductase
Function
Catalyzes the hydroxylation of L-kynurenine (L-Kyn) to form 3-hydroxy-L-kynurenine (L-3OHKyn) (PubMed:29429898, PubMed:23575632, PubMed:26752518, PubMed:28604669, PubMed:29208702). Required for synthesis of quinolinic acid, a neurotoxic NMDA receptor antagonist and potential endogenous inhibitor of NMDA receptor signaling in axonal targeting, synaptogenesis and apoptosis during brain development. Quinolinic acid may also affect NMDA receptor signaling in pancreatic beta cells, osteoblasts, myocardial cells, and the gastrointestinal tract (Probable).
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Uniprot ID
Primary ID:
O15229

Secondarily ID:
A2A2U8
A2A2U9
A2A2V0
Q5SY07
Q5SY08
Q5SY09
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Ensembl ID
ENSG00000117009
HGNC ID
HGNC:6381
Subcellular Location
Mitochondrion outer 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: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0072068
6-(3-chloro-4-cyclopropyloxyphenyl)pyrimidine-4-carboxylic acid
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C14H11ClN2O3
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0116248
6-[3-chloro-4-(trifluoromethoxy)phenyl]pyrimidine-4-carboxylic acid
   Show/Hide
C12H6ClF3N2O3
 1
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0246794
6-(4-chloro-3-fluorophenyl)pyrimidine-4-carboxylic acid
   Show/Hide
C11H6ClFN2O2
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0148175
6-(3-chloro-4-methoxyphenyl)pyrimidine-4-carboxylic acid
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C12H9ClN2O3
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0069400
6-(1-benzofuran-5-yl)pyrimidine-4-carboxylic acid
   Show/Hide
C13H8N2O3
 1
1
IC50 = 21 nM
   TI
   LI
   LO
   TS
CP0120388
6-(3-chloro-4-propan-2-yloxyphenyl)pyrimidine-4-carboxylic acid
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C14H13ClN2O3
 1
1
IC50 = 23 nM
   TI
   LI
   LO
   TS
CP0088950
6-(3-chloro-4-cyclobutyloxyphenyl)pyrimidine-4-carboxylic acid
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C15H13ClN2O3
 1
1
IC50 = 24 nM
   TI
   LI
   LO
   TS
CP0069422
6-(3-chloro-4-methylphenyl)pyrimidine-4-carboxylic acid
   Show/Hide
C12H9ClN2O2
 1
1
IC50 = 26 nM
   TI
   LI
   LO
   TS
CP0116249
6-(3,4-dichlorophenyl)pyrimidine-4-carboxylic acid
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C11H6Cl2N2O2
 1
1
IC50 = 33 nM
   TI
   LI
   LO
   TS
CP0089959
6-(3,4-difluorophenyl)pyrimidine-4-carboxylic acid
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C11H6F2N2O2
 1
1
IC50 = 38 nM
   TI
   LI
   LO
   TS
CP0055820
6-(3-chloro-4-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
 1
1
IC50 = 52 nM
   TI
   LI
   LO
   TS
CP0177538
3-[6-(3,4-dichlorophenyl)pyrimidin-4-yl]-4H-1,2,4-oxadiazol-5-one
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C12H6Cl2N4O2
 1
1
IC50 = 60 nM
   TI
   LI
   LO
   TS
CP0148177
6-(3-chloro-4-cyclopentyloxyphenyl)pyrimidine-4-carboxylic acid
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C16H15ClN2O3
 1
1
IC50 = 64 nM
   TI
   LI
   LO
   TS
CP0132482
N-(benzenesulfonyl)-6-(3,4-dichlorophenyl)pyrimidine-4-carboxamide
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C17H11Cl2N3O3S
 1
1
IC50 = 72.6 nM
   TI
   LI
   LO
   TS
CP0334849
6-[3-chloro-4-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
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C12H6ClF3N2O2
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0148170
4-(3,4-dichlorophenyl)pyridine-2-carboxylic acid
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C12H7Cl2NO2
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0358461
6-(4-chlorophenyl)pyrimidine-4-carboxylic acid
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C11H7ClN2O2
 1
1
IC50 = 210 nM
   TI
   LI
   LO
   TS
CP0089956
4-(3,4-dichlorophenyl)-6-(2H-tetrazol-5-yl)pyrimidine
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C11H6Cl2N6
 1
1
IC50 = 230 nM
   TI
   LI
   LO
   TS
CP0088949
6-[3-chloro-4-(cyclopropylmethoxy)phenyl]pyrimidine-4-carboxylic acid
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C15H13ClN2O3
 1
1
IC50 = 270 nM
   TI
   LI
   LO
   TS
CP0060274
6-(3-chlorophenyl)pyrimidine-4-carboxylic acid
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C11H7ClN2O2
 1
1
IC50 = 290 nM
   TI
   LI
   LO
   TS
CP0177535
6-(3,4-dichlorophenyl)-2-methylpyrimidine-4-carboxylic acid
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C12H8Cl2N2O2
 1
1
IC50 = 300 nM
   TI
   LI
   LO
   TS
CP0088947
6-(3-chloro-2-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
 1
1
IC50 = 310 nM
   TI
   LI
   LO
   TS
CP0387241
6-(3,5-dichlorophenyl)pyrimidine-4-carboxylic acid
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C11H6Cl2N2O2
 1
1
IC50 = 320 nM
   TI
   LI
   LO
   TS
CP0069399
6-(3-chloro-4-pyrrolidin-1-ylphenyl)pyrimidine-4-carboxylic acid
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C15H14ClN3O2
 1
1
IC50 = 350 nM
   TI
   LI
   LO
   TS
CP0310582
6-(3-fluoro-4-methylphenyl)pyrimidine-4-carboxylic acid
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C12H9FN2O2
 1
1
IC50 = 370 nM
   TI
   LI
   LO
   TS
CP0055822
6-[3-chloro-4-(oxetan-3-yloxy)phenyl]pyrimidine-4-carboxylic acid
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C14H11ClN2O4
 1
1
IC50 = 520 nM
   TI
   LI
   LO
   TS
CP0148173
N-[6-(3,4-dichlorophenyl)pyrimidin-4-yl]benzenesulfonamide
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C16H11Cl2N3O2S
 1
1
IC50 = 590 nM
   TI
   LI
   LO
   TS
CP0088946
6-(3-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H7FN2O2
 1
1
IC50 = 690 nM
   TI
   LI
   LO
   TS
CP0327344
2-(3,4-dichlorophenyl)pyridine-4-carboxylic acid
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C12H7Cl2NO2
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0148172
6-(3,4-dichlorophenyl)-5-methylpyrimidine-4-carboxylic acid
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C12H8Cl2N2O2
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0088948
6-(4-chloro-2-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
 1
1
IC50 = 1740 nM
   TI
   LI
   LO
   TS
CP0177536
6-(3,4-dichlorophenyl)-5-hydroxypyrimidine-4-carboxylic acid
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C11H6Cl2N2O3
 1
1
IC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0089961
6-[3-chloro-4-(2-morpholin-4-ylethoxy)phenyl]pyrimidine-4-carboxylic acid
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C17H18ClN3O4
 1
1
IC50 = 4300 nM
   TI
   LI
   LO
   TS
CP0171214
6-(3,4-dichlorophenyl)-5-(methoxymethyl)pyrimidine-4-carboxylic acid
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C13H10Cl2N2O3
 1
1
IC50 = 4300 nM
   TI
   LI
   LO
   TS
CP0132480
6-(3,4-dichlorophenyl)-5-methoxypyrimidine-4-carboxylic acid
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C12H8Cl2N2O3
 1
1
IC50 = 4400 nM
   TI
   LI
   LO
   TS
CP0046937
5-amino-6-(3,4-dichlorophenyl)pyrimidine-4-carboxylic acid
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C11H7Cl2N3O2
 1
1
IC50 = 5500 nM
   TI
   LI
   LO
   TS
CP0132485
6-(2,4-difluorophenyl)pyrimidine-4-carboxylic acid
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C11H6F2N2O2
 1
1
IC50 = 7220 nM
   TI
   LI
   LO
   TS
CP0310580
6-(3-methylphenyl)pyrimidine-4-carboxylic acid
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C12H10N2O2
 1
1
IC50 = 7500 nM
   TI
   LI
   LO
   TS
CP0072006
6-(3,4-dichlorophenyl)-5-fluoropyrimidine-4-carboxylic acid
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C11H5Cl2FN2O2
 1
1
IC50 = 9200 nM
   TI
   LI
   LO
   TS
CP0116241
6-pyridin-3-ylpyrimidine-4-carboxylic acid
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C10H7N3O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0120387
6-[4-fluoro-3-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
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C12H6F4N2O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0148168
6-morpholin-4-ylpyrimidine-4-carboxylic acid
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C9H11N3O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0148169
6-(3,4-dichlorophenoxy)pyrimidine-4-carboxylic acid
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C11H6Cl2N2O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0177539
6-[4-chloro-3-(2-morpholin-4-ylethoxy)phenyl]pyrimidine-4-carboxylic acid
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C17H18ClN3O4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0180375
6-phenylpyrimidine-4-carboxylic acid
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C11H8N2O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0272700
6-[2-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
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C12H7F3N2O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0283407
6-(3,4-dichloroanilino)pyrimidine-4-carboxylic acid
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C11H7Cl2N3O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0310579
6-[3-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
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C12H7F3N2O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0327357
6-(4-chloro-3-methoxyphenyl)pyrimidine-4-carboxylic acid
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C12H9ClN2O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0337721
6-(3-phenylphenyl)pyrimidine-4-carboxylic acid
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C17H12N2O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0358460
6-cyclohexylpyrimidine-4-carboxylic acid
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C11H14N2O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0088947
6-(3-chloro-2-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
 1
1 IC50 = 0.2 nM
CP0089959
6-(3,4-difluorophenyl)pyrimidine-4-carboxylic acid
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C11H6F2N2O2
 2
1 IC50 = 0.2 nM
2 IC50 = 62 nM
CP0088946
6-(3-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H7FN2O2
 1
1 IC50 = 0.3 nM
CP0246794
6-(4-chloro-3-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
 1
1 IC50 = 0.3 nM
CP0060274
6-(3-chlorophenyl)pyrimidine-4-carboxylic acid
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C11H7ClN2O2
 1
1 IC50 = 0.5 nM
CP0072068
6-(3-chloro-4-cyclopropyloxyphenyl)pyrimidine-4-carboxylic acid
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C14H11ClN2O3
 2
1 IC50 = 0.5 nM
2 IC50 = 82 nM
CP0116249
6-(3,4-dichlorophenyl)pyrimidine-4-carboxylic acid
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C11H6Cl2N2O2
 2
1 IC50 = 0.6 nM
2 IC50 = 72 nM
CP0069422
6-(3-chloro-4-methylphenyl)pyrimidine-4-carboxylic acid
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C12H9ClN2O2
 2
1 IC50 = 0.7 nM
2 IC50 = 140 nM
CP0055820
6-(3-chloro-4-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
 1
1 IC50 = 0.9 nM
CP0310582
6-(3-fluoro-4-methylphenyl)pyrimidine-4-carboxylic acid
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C12H9FN2O2
 1
1 IC50 = 0.9 nM
CP0148175
6-(3-chloro-4-methoxyphenyl)pyrimidine-4-carboxylic acid
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C12H9ClN2O3
 1
1 IC50 = 1.2 nM
CP0069400
6-(1-benzofuran-5-yl)pyrimidine-4-carboxylic acid
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C13H8N2O3
 1
1 IC50 = 1.5 nM
CP0055822
6-[3-chloro-4-(oxetan-3-yloxy)phenyl]pyrimidine-4-carboxylic acid
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C14H11ClN2O4
 1
1 IC50 = 2 nM
CP0089956
4-(3,4-dichlorophenyl)-6-(2H-tetrazol-5-yl)pyrimidine
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C11H6Cl2N6
 1
1 IC50 = 2 nM
CP0116248
6-[3-chloro-4-(trifluoromethoxy)phenyl]pyrimidine-4-carboxylic acid
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C12H6ClF3N2O3
 2
1 IC50 = 2.1 nM
2 IC50 = 115 nM
CP0148170
4-(3,4-dichlorophenyl)pyridine-2-carboxylic acid
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C12H7Cl2NO2
 1
1 IC50 = 3.2 nM
CP0334849
6-[3-chloro-4-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
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C12H6ClF3N2O2
 1
1 IC50 = 5 nM
CP0072006
6-(3,4-dichlorophenyl)-5-fluoropyrimidine-4-carboxylic acid
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C11H5Cl2FN2O2
 1
1 IC50 = 6 nM
CP0120388
6-(3-chloro-4-propan-2-yloxyphenyl)pyrimidine-4-carboxylic acid
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C14H13ClN2O3
 1
1 IC50 = 6 nM
CP0148172
6-(3,4-dichlorophenyl)-5-methylpyrimidine-4-carboxylic acid
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C12H8Cl2N2O2
 1
1 IC50 = 10 nM
CP0358461
6-(4-chlorophenyl)pyrimidine-4-carboxylic acid
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C11H7ClN2O2
 1
1 IC50 = 11 nM
CP0088950
6-(3-chloro-4-cyclobutyloxyphenyl)pyrimidine-4-carboxylic acid
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C15H13ClN2O3
 1
1 IC50 = 12 nM
CP0177535
6-(3,4-dichlorophenyl)-2-methylpyrimidine-4-carboxylic acid
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C12H8Cl2N2O2
 1
1 IC50 = 12 nM
CP0177538
3-[6-(3,4-dichlorophenyl)pyrimidin-4-yl]-4H-1,2,4-oxadiazol-5-one
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C12H6Cl2N4O2
 1
1 IC50 = 12 nM
CP0310580
6-(3-methylphenyl)pyrimidine-4-carboxylic acid
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C12H10N2O2
 1
1 IC50 = 17 nM
CP0387241
6-(3,5-dichlorophenyl)pyrimidine-4-carboxylic acid
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C11H6Cl2N2O2
 1
1 IC50 = 19 nM
CP0310579
6-[3-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
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C12H7F3N2O2
 1
1 IC50 = 22 nM
CP0132482
N-(benzenesulfonyl)-6-(3,4-dichlorophenyl)pyrimidine-4-carboxamide
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C17H11Cl2N3O3S
 1
1 IC50 = 25 nM
CP0120387
6-[4-fluoro-3-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
   Show/Hide
C12H6F4N2O2
 1
1 IC50 = 32 nM
CP0171214
6-(3,4-dichlorophenyl)-5-(methoxymethyl)pyrimidine-4-carboxylic acid
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C13H10Cl2N2O3
 1
1 IC50 = 33 nM
CP0088948
6-(4-chloro-2-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
 1
1 IC50 = 38 nM
CP0180375
6-phenylpyrimidine-4-carboxylic acid
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C11H8N2O2
 1
1 IC50 = 38 nM
CP0132480
6-(3,4-dichlorophenyl)-5-methoxypyrimidine-4-carboxylic acid
   Show/Hide
C12H8Cl2N2O3
 1
1 IC50 = 40 nM
CP0088949
6-[3-chloro-4-(cyclopropylmethoxy)phenyl]pyrimidine-4-carboxylic acid
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C15H13ClN2O3
 1
1 IC50 = 49 nM
CP0148177
6-(3-chloro-4-cyclopentyloxyphenyl)pyrimidine-4-carboxylic acid
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C16H15ClN2O3
 1
1 IC50 = 57 nM
CP0327357
6-(4-chloro-3-methoxyphenyl)pyrimidine-4-carboxylic acid
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C12H9ClN2O3
 1
1 IC50 = 60 nM
CP0132485
6-(2,4-difluorophenyl)pyrimidine-4-carboxylic acid
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C11H6F2N2O2
 1
1 IC50 = 76 nM
CP0089961
6-[3-chloro-4-(2-morpholin-4-ylethoxy)phenyl]pyrimidine-4-carboxylic acid
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C17H18ClN3O4
 1
1 IC50 = 83 nM
CP0327344
2-(3,4-dichlorophenyl)pyridine-4-carboxylic acid
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C12H7Cl2NO2
 1
1 IC50 = 90 nM
CP0177536
6-(3,4-dichlorophenyl)-5-hydroxypyrimidine-4-carboxylic acid
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C11H6Cl2N2O3
 1
1 IC50 = 140 nM
CP0046937
5-amino-6-(3,4-dichlorophenyl)pyrimidine-4-carboxylic acid
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C11H7Cl2N3O2
 1
1 IC50 = 260 nM
CP0148173
N-[6-(3,4-dichlorophenyl)pyrimidin-4-yl]benzenesulfonamide
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C16H11Cl2N3O2S
 1
1 IC50 = 270 nM
CP0358460
6-cyclohexylpyrimidine-4-carboxylic acid
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C11H14N2O2
 1
1 IC50 = 340 nM
CP0069399
6-(3-chloro-4-pyrrolidin-1-ylphenyl)pyrimidine-4-carboxylic acid
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C15H14ClN3O2
 1
1 IC50 = 550 nM
CP0116241
6-pyridin-3-ylpyrimidine-4-carboxylic acid
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C10H7N3O2
 1
1 IC50 = 990 nM
CP0148169
6-(3,4-dichlorophenoxy)pyrimidine-4-carboxylic acid
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C11H6Cl2N2O3
 1
1 IC50 = 1300 nM
CP0177539
6-[4-chloro-3-(2-morpholin-4-ylethoxy)phenyl]pyrimidine-4-carboxylic acid
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C17H18ClN3O4
 1
1 IC50 = 2050 nM
CP0337721
6-(3-phenylphenyl)pyrimidine-4-carboxylic acid
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C17H12N2O2
 1
1 IC50 = 2130 nM
CP0272700
6-[2-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
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C12H7F3N2O2
 1
1 IC50 = 6510 nM
CP0283407
6-(3,4-dichloroanilino)pyrimidine-4-carboxylic acid
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C11H7Cl2N3O2
 1
1 IC50 = 9500 nM
CP0148168
6-morpholin-4-ylpyrimidine-4-carboxylic acid
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C9H11N3O3
 1
1 IC50 = 16700 nM
CP0065196
3-[5-chloro-2-oxo-6-[(1R)-1-pyridazin-3-ylethoxy]-1,3-benzoxazol-3-yl]propanoic acid
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C16H14ClN3O5
 1
1 IC50 < 794.33 nM
Clinical Information about the Protein
Target 1 ( Kynurenine 3-hydroxylase (KMO) )
Target Type Clinical trial Target
Disease 2 Target-related Diseases  2
1 Pancreatitis [ICD-11: DC31-DC34]
2 Neurodegenerative disorder [ICD-11: 8A20-8A23]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 GSK065 Phase 1
Pancreatitis
Preclinical Drug(s) 4 Preclinical Drugs  4
1 GSK180 Preclinical
Neurodegenerative disorder
2 GSK366 Preclinical
Pancreatitis
3 Ro 61-8048 Preclinical
Neurodegenerative disorder
4 UPF-648 Preclinical
Neurodegenerative disorder