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Literature summary for 2.5.1.47 extracted from

  • Brunner, K.; Steiner, E.M.; Reshma, R.S.; Sriram, D.; Schnell, R.; Schneider, G.
    Profiling of in vitro activities of urea-based inhibitors against cysteine synthases from Mycobacterium tuberculosis (2017), Bioorg. Med. Chem. Lett., 27, 4582-4587 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3-[[(3,4-dichlorophenyl)carbamoyl]amino]benzoic acid inhibits both isoforms CysK1 and CysK2 and O-phosphoserine sulfhydrylase CysM Mycobacterium tuberculosis
3-[[([1,1'-biphenyl]-3-yl)carbamoyl]amino]benzoic acid inhibits both isoforms CysK1 and CysK2 and O-phosphoserine sulfhydrylase CysM Mycobacterium tuberculosis
4-[[(3,4-dichlorophenyl)carbamoyl]amino]-2-hydroxybenzoic acid selective for isoform CysK1, IC50 value for isoform CysK2 above 300 microM Mycobacterium tuberculosis
4-[[([1,1'-biphenyl]-3-yl)carbamoyl]amino]-2-hydroxybenzoic acid inhibits both isoforms CysK1 and CysK2 and O-phosphoserine sulfhydrylase CysM Mycobacterium tuberculosis
5-[[(3,4-dichlorophenyl)carbamoyl]amino]-2-hydroxybenzoic acid inhibits both isoforms CysK1 and CysK2 Mycobacterium tuberculosis
5-[[([1,1'-biphenyl]-3-yl)carbamoyl]amino]-2-hydroxybenzoic acid inhibits both isoforms CysK1 and CysK2 and O-phosphoserine sulfhydrylase CysM Mycobacterium tuberculosis

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis Q79FV4 isoform CysK2
-
Mycobacterium tuberculosis ATCC 25618 Q79FV4 isoform CysK2
-

Synonyms

Synonyms Comment Organism
CysK2
-
Mycobacterium tuberculosis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0066
-
pH not specified in the publication, temperature not specified in the publication Mycobacterium tuberculosis 3-[[([1,1'-biphenyl]-3-yl)carbamoyl]amino]benzoic acid
0.0101
-
pH not specified in the publication, temperature not specified in the publication Mycobacterium tuberculosis 3-[[(3,4-dichlorophenyl)carbamoyl]amino]benzoic acid
0.0103
-
pH not specified in the publication, temperature not specified in the publication Mycobacterium tuberculosis 5-[[([1,1'-biphenyl]-3-yl)carbamoyl]amino]-2-hydroxybenzoic acid
0.0269
-
pH not specified in the publication, temperature not specified in the publication Mycobacterium tuberculosis 4-[[([1,1'-biphenyl]-3-yl)carbamoyl]amino]-2-hydroxybenzoic acid
0.0299
-
pH not specified in the publication, temperature not specified in the publication Mycobacterium tuberculosis 5-[[(3,4-dichlorophenyl)carbamoyl]amino]-2-hydroxybenzoic acid