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
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0072068
 Compound Info 
6-(3-chloro-4-cyclopropyloxyphenyl)pyrimidine-4-carboxylic acid
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C14H11ClN2O3
  1
1
IC50 = 8 nM
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CP0116248
 Compound Info 
6-[3-chloro-4-(trifluoromethoxy)phenyl]pyrimidine-4-carboxylic acid
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C12H6ClF3N2O3
  1
1
IC50 = 11 nM
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CP0246794
 Compound Info 
6-(4-chloro-3-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
  1
1
IC50 = 13 nM
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CP0148175
 Compound Info 
6-(3-chloro-4-methoxyphenyl)pyrimidine-4-carboxylic acid
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C12H9ClN2O3
  1
1
IC50 = 16 nM
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CP0069400
 Compound Info 
6-(1-benzofuran-5-yl)pyrimidine-4-carboxylic acid
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C13H8N2O3
  1
1
IC50 = 21 nM
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CP0120388
 Compound Info 
6-(3-chloro-4-propan-2-yloxyphenyl)pyrimidine-4-carboxylic acid
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C14H13ClN2O3
  1
1
IC50 = 23 nM
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CP0088950
 Compound Info 
6-(3-chloro-4-cyclobutyloxyphenyl)pyrimidine-4-carboxylic acid
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C15H13ClN2O3
  1
1
IC50 = 24 nM
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CP0069422
 Compound Info 
6-(3-chloro-4-methylphenyl)pyrimidine-4-carboxylic acid
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C12H9ClN2O2
  1
1
IC50 = 26 nM
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CP0116249
 Compound Info 
6-(3,4-dichlorophenyl)pyrimidine-4-carboxylic acid
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C11H6Cl2N2O2
  1
1
IC50 = 33 nM
 Bioactivity Info 
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CP0089959
 Compound Info 
6-(3,4-difluorophenyl)pyrimidine-4-carboxylic acid
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C11H6F2N2O2
  1
1
IC50 = 38 nM
 Bioactivity Info 
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CP0055820
 Compound Info 
6-(3-chloro-4-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
  1
1
IC50 = 52 nM
 Bioactivity Info 
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CP0177538
 Compound Info 
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
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CP0148177
 Compound Info 
6-(3-chloro-4-cyclopentyloxyphenyl)pyrimidine-4-carboxylic acid
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C16H15ClN2O3
  1
1
IC50 = 64 nM
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CP0132482
 Compound Info 
N-(benzenesulfonyl)-6-(3,4-dichlorophenyl)pyrimidine-4-carboxamide
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C17H11Cl2N3O3S
  1
1
IC50 = 72.6 nM
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CP0334849
 Compound Info 
6-[3-chloro-4-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
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C12H6ClF3N2O2
  1
1
IC50 = 120 nM
 Bioactivity Info 
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CP0148170
 Compound Info 
4-(3,4-dichlorophenyl)pyridine-2-carboxylic acid
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C12H7Cl2NO2
  1
1
IC50 = 170 nM
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CP0358461
 Compound Info 
6-(4-chlorophenyl)pyrimidine-4-carboxylic acid
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C11H7ClN2O2
  1
1
IC50 = 210 nM
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CP0089956
 Compound Info 
4-(3,4-dichlorophenyl)-6-(2H-tetrazol-5-yl)pyrimidine
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C11H6Cl2N6
  1
1
IC50 = 230 nM
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CP0088949
 Compound Info 
6-[3-chloro-4-(cyclopropylmethoxy)phenyl]pyrimidine-4-carboxylic acid
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C15H13ClN2O3
  1
1
IC50 = 270 nM
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CP0060274
 Compound Info 
6-(3-chlorophenyl)pyrimidine-4-carboxylic acid
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C11H7ClN2O2
  1
1
IC50 = 290 nM
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CP0177535
 Compound Info 
6-(3,4-dichlorophenyl)-2-methylpyrimidine-4-carboxylic acid
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C12H8Cl2N2O2
  1
1
IC50 = 300 nM
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CP0088947
 Compound Info 
6-(3-chloro-2-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
  1
1
IC50 = 310 nM
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CP0387241
 Compound Info 
6-(3,5-dichlorophenyl)pyrimidine-4-carboxylic acid
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C11H6Cl2N2O2
  1
1
IC50 = 320 nM
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CP0069399
 Compound Info 
6-(3-chloro-4-pyrrolidin-1-ylphenyl)pyrimidine-4-carboxylic acid
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C15H14ClN3O2
  1
1
IC50 = 350 nM
 Bioactivity Info 
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CP0310582
 Compound Info 
6-(3-fluoro-4-methylphenyl)pyrimidine-4-carboxylic acid
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C12H9FN2O2
  1
1
IC50 = 370 nM
 Bioactivity Info 
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CP0055822
 Compound Info 
6-[3-chloro-4-(oxetan-3-yloxy)phenyl]pyrimidine-4-carboxylic acid
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C14H11ClN2O4
  1
1
IC50 = 520 nM
 Bioactivity Info 
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CP0148173
 Compound Info 
N-[6-(3,4-dichlorophenyl)pyrimidin-4-yl]benzenesulfonamide
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C16H11Cl2N3O2S
  1
1
IC50 = 590 nM
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CP0088946
 Compound Info 
6-(3-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H7FN2O2
  1
1
IC50 = 690 nM
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CP0327344
 Compound Info 
2-(3,4-dichlorophenyl)pyridine-4-carboxylic acid
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C12H7Cl2NO2
  1
1
IC50 = 1100 nM
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CP0148172
 Compound Info 
6-(3,4-dichlorophenyl)-5-methylpyrimidine-4-carboxylic acid
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C12H8Cl2N2O2
  1
1
IC50 = 1500 nM
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CP0088948
 Compound Info 
6-(4-chloro-2-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
  1
1
IC50 = 1740 nM
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CP0177536
 Compound Info 
6-(3,4-dichlorophenyl)-5-hydroxypyrimidine-4-carboxylic acid
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C11H6Cl2N2O3
  1
1
IC50 = 3500 nM
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CP0089961
 Compound Info 
6-[3-chloro-4-(2-morpholin-4-ylethoxy)phenyl]pyrimidine-4-carboxylic acid
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C17H18ClN3O4
  1
1
IC50 = 4300 nM
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CP0171214
 Compound Info 
6-(3,4-dichlorophenyl)-5-(methoxymethyl)pyrimidine-4-carboxylic acid
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C13H10Cl2N2O3
  1
1
IC50 = 4300 nM
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CP0132480
 Compound Info 
6-(3,4-dichlorophenyl)-5-methoxypyrimidine-4-carboxylic acid
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C12H8Cl2N2O3
  1
1
IC50 = 4400 nM
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CP0046937
 Compound Info 
5-amino-6-(3,4-dichlorophenyl)pyrimidine-4-carboxylic acid
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C11H7Cl2N3O2
  1
1
IC50 = 5500 nM
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CP0132485
 Compound Info 
6-(2,4-difluorophenyl)pyrimidine-4-carboxylic acid
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C11H6F2N2O2
  1
1
IC50 = 7220 nM
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CP0310580
 Compound Info 
6-(3-methylphenyl)pyrimidine-4-carboxylic acid
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C12H10N2O2
  1
1
IC50 = 7500 nM
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CP0072006
 Compound Info 
6-(3,4-dichlorophenyl)-5-fluoropyrimidine-4-carboxylic acid
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C11H5Cl2FN2O2
  1
1
IC50 = 9200 nM
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CP0116241
 Compound Info 
6-pyridin-3-ylpyrimidine-4-carboxylic acid
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C10H7N3O2
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0120387
 Compound Info 
6-[4-fluoro-3-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
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C12H6F4N2O2
  1
1
IC50 > 10000 nM
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CP0148168
 Compound Info 
6-morpholin-4-ylpyrimidine-4-carboxylic acid
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C9H11N3O3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0148169
 Compound Info 
6-(3,4-dichlorophenoxy)pyrimidine-4-carboxylic acid
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C11H6Cl2N2O3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0177539
 Compound Info 
6-[4-chloro-3-(2-morpholin-4-ylethoxy)phenyl]pyrimidine-4-carboxylic acid
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C17H18ClN3O4
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0180375
 Compound Info 
6-phenylpyrimidine-4-carboxylic acid
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C11H8N2O2
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0272700
 Compound Info 
6-[2-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
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C12H7F3N2O2
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0283407
 Compound Info 
6-(3,4-dichloroanilino)pyrimidine-4-carboxylic acid
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C11H7Cl2N3O2
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0310579
 Compound Info 
6-[3-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
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C12H7F3N2O2
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0327357
 Compound Info 
6-(4-chloro-3-methoxyphenyl)pyrimidine-4-carboxylic acid
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C12H9ClN2O3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0337721
 Compound Info 
6-(3-phenylphenyl)pyrimidine-4-carboxylic acid
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C17H12N2O2
  1
1
IC50 > 10000 nM
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CP0358460
 Compound Info 
6-cyclohexylpyrimidine-4-carboxylic acid
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C11H14N2O2
  1
1
IC50 > 10000 nM
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Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0088947
 Compound Info 
6-(3-chloro-2-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
  1
1 IC50 = 0.2 nM
CP0089959
 Compound Info 
6-(3,4-difluorophenyl)pyrimidine-4-carboxylic acid
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C11H6F2N2O2
  2
1 IC50 = 0.2 nM
2 IC50 = 62 nM
CP0088946
 Compound Info 
6-(3-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H7FN2O2
  1
1 IC50 = 0.3 nM
CP0246794
 Compound Info 
6-(4-chloro-3-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
  1
1 IC50 = 0.3 nM
CP0060274
 Compound Info 
6-(3-chlorophenyl)pyrimidine-4-carboxylic acid
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C11H7ClN2O2
  1
1 IC50 = 0.5 nM
CP0072068
 Compound Info 
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
 Compound Info 
6-(3,4-dichlorophenyl)pyrimidine-4-carboxylic acid
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C11H6Cl2N2O2
  2
1 IC50 = 0.6 nM
2 IC50 = 72 nM
CP0069422
 Compound Info 
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
 Compound Info 
6-(3-chloro-4-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
  1
1 IC50 = 0.9 nM
CP0310582
 Compound Info 
6-(3-fluoro-4-methylphenyl)pyrimidine-4-carboxylic acid
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C12H9FN2O2
  1
1 IC50 = 0.9 nM
CP0148175
 Compound Info 
6-(3-chloro-4-methoxyphenyl)pyrimidine-4-carboxylic acid
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C12H9ClN2O3
  1
1 IC50 = 1.2 nM
CP0069400
 Compound Info 
6-(1-benzofuran-5-yl)pyrimidine-4-carboxylic acid
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C13H8N2O3
  1
1 IC50 = 1.5 nM
CP0055822
 Compound Info 
6-[3-chloro-4-(oxetan-3-yloxy)phenyl]pyrimidine-4-carboxylic acid
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C14H11ClN2O4
  1
1 IC50 = 2 nM
CP0089956
 Compound Info 
4-(3,4-dichlorophenyl)-6-(2H-tetrazol-5-yl)pyrimidine
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C11H6Cl2N6
  1
1 IC50 = 2 nM
CP0116248
 Compound Info 
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
 Compound Info 
4-(3,4-dichlorophenyl)pyridine-2-carboxylic acid
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C12H7Cl2NO2
  1
1 IC50 = 3.2 nM
CP0334849
 Compound Info 
6-[3-chloro-4-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
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C12H6ClF3N2O2
  1
1 IC50 = 5 nM
CP0072006
 Compound Info 
6-(3,4-dichlorophenyl)-5-fluoropyrimidine-4-carboxylic acid
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C11H5Cl2FN2O2
  1
1 IC50 = 6 nM
CP0120388
 Compound Info 
6-(3-chloro-4-propan-2-yloxyphenyl)pyrimidine-4-carboxylic acid
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C14H13ClN2O3
  1
1 IC50 = 6 nM
CP0148172
 Compound Info 
6-(3,4-dichlorophenyl)-5-methylpyrimidine-4-carboxylic acid
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C12H8Cl2N2O2
  1
1 IC50 = 10 nM
CP0358461
 Compound Info 
6-(4-chlorophenyl)pyrimidine-4-carboxylic acid
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C11H7ClN2O2
  1
1 IC50 = 11 nM
CP0088950
 Compound Info 
6-(3-chloro-4-cyclobutyloxyphenyl)pyrimidine-4-carboxylic acid
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C15H13ClN2O3
  1
1 IC50 = 12 nM
CP0177535
 Compound Info 
6-(3,4-dichlorophenyl)-2-methylpyrimidine-4-carboxylic acid
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C12H8Cl2N2O2
  1
1 IC50 = 12 nM
CP0177538
 Compound Info 
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
 Compound Info 
6-(3-methylphenyl)pyrimidine-4-carboxylic acid
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C12H10N2O2
  1
1 IC50 = 17 nM
CP0387241
 Compound Info 
6-(3,5-dichlorophenyl)pyrimidine-4-carboxylic acid
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C11H6Cl2N2O2
  1
1 IC50 = 19 nM
CP0310579
 Compound Info 
6-[3-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
   Show/Hide
C12H7F3N2O2
  1
1 IC50 = 22 nM
CP0132482
 Compound Info 
N-(benzenesulfonyl)-6-(3,4-dichlorophenyl)pyrimidine-4-carboxamide
   Show/Hide
C17H11Cl2N3O3S
  1
1 IC50 = 25 nM
CP0120387
 Compound Info 
6-[4-fluoro-3-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
   Show/Hide
C12H6F4N2O2
  1
1 IC50 = 32 nM
CP0171214
 Compound Info 
6-(3,4-dichlorophenyl)-5-(methoxymethyl)pyrimidine-4-carboxylic acid
   Show/Hide
C13H10Cl2N2O3
  1
1 IC50 = 33 nM
CP0088948
 Compound Info 
6-(4-chloro-2-fluorophenyl)pyrimidine-4-carboxylic acid
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C11H6ClFN2O2
  1
1 IC50 = 38 nM
CP0180375
 Compound Info 
6-phenylpyrimidine-4-carboxylic acid
   Show/Hide
C11H8N2O2
  1
1 IC50 = 38 nM
CP0132480
 Compound Info 
6-(3,4-dichlorophenyl)-5-methoxypyrimidine-4-carboxylic acid
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C12H8Cl2N2O3
  1
1 IC50 = 40 nM
CP0088949
 Compound Info 
6-[3-chloro-4-(cyclopropylmethoxy)phenyl]pyrimidine-4-carboxylic acid
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C15H13ClN2O3
  1
1 IC50 = 49 nM
CP0148177
 Compound Info 
6-(3-chloro-4-cyclopentyloxyphenyl)pyrimidine-4-carboxylic acid
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C16H15ClN2O3
  1
1 IC50 = 57 nM
CP0327357
 Compound Info 
6-(4-chloro-3-methoxyphenyl)pyrimidine-4-carboxylic acid
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C12H9ClN2O3
  1
1 IC50 = 60 nM
CP0132485
 Compound Info 
6-(2,4-difluorophenyl)pyrimidine-4-carboxylic acid
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C11H6F2N2O2
  1
1 IC50 = 76 nM
CP0089961
 Compound Info 
6-[3-chloro-4-(2-morpholin-4-ylethoxy)phenyl]pyrimidine-4-carboxylic acid
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C17H18ClN3O4
  1
1 IC50 = 83 nM
CP0327344
 Compound Info 
2-(3,4-dichlorophenyl)pyridine-4-carboxylic acid
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C12H7Cl2NO2
  1
1 IC50 = 90 nM
CP0177536
 Compound Info 
6-(3,4-dichlorophenyl)-5-hydroxypyrimidine-4-carboxylic acid
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C11H6Cl2N2O3
  1
1 IC50 = 140 nM
CP0046937
 Compound Info 
5-amino-6-(3,4-dichlorophenyl)pyrimidine-4-carboxylic acid
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C11H7Cl2N3O2
  1
1 IC50 = 260 nM
CP0148173
 Compound Info 
N-[6-(3,4-dichlorophenyl)pyrimidin-4-yl]benzenesulfonamide
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C16H11Cl2N3O2S
  1
1 IC50 = 270 nM
CP0358460
 Compound Info 
6-cyclohexylpyrimidine-4-carboxylic acid
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C11H14N2O2
  1
1 IC50 = 340 nM
CP0069399
 Compound Info 
6-(3-chloro-4-pyrrolidin-1-ylphenyl)pyrimidine-4-carboxylic acid
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C15H14ClN3O2
  1
1 IC50 = 550 nM
CP0116241
 Compound Info 
6-pyridin-3-ylpyrimidine-4-carboxylic acid
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C10H7N3O2
  1
1 IC50 = 990 nM
CP0148169
 Compound Info 
6-(3,4-dichlorophenoxy)pyrimidine-4-carboxylic acid
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C11H6Cl2N2O3
  1
1 IC50 = 1300 nM
CP0177539
 Compound Info 
6-[4-chloro-3-(2-morpholin-4-ylethoxy)phenyl]pyrimidine-4-carboxylic acid
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C17H18ClN3O4
  1
1 IC50 = 2050 nM
CP0337721
 Compound Info 
6-(3-phenylphenyl)pyrimidine-4-carboxylic acid
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C17H12N2O2
  1
1 IC50 = 2130 nM
CP0272700
 Compound Info 
6-[2-(trifluoromethyl)phenyl]pyrimidine-4-carboxylic acid
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C12H7F3N2O2
  1
1 IC50 = 6510 nM
CP0283407
 Compound Info 
6-(3,4-dichloroanilino)pyrimidine-4-carboxylic acid
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C11H7Cl2N3O2
  1
1 IC50 = 9500 nM
CP0148168
 Compound Info 
6-morpholin-4-ylpyrimidine-4-carboxylic acid
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C9H11N3O3
  1
1 IC50 = 16700 nM
CP0065196
 Compound Info 
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
 Drug Info 
Phase 1
Pancreatitis
Preclinical Drug(s) 4 Preclinical Drugs  4
1 GSK180
 Drug Info 
Preclinical
Neurodegenerative disorder
2 GSK366
 Drug Info 
Preclinical
Pancreatitis
3 Ro 61-8048
 Drug Info 
Preclinical
Neurodegenerative disorder
4 UPF-648
 Drug Info 
Preclinical
Neurodegenerative disorder