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Literature summary for 2.7.11.1 extracted from

  • Hawkinson, J.; Sinville, R.; Mudaliar, D.; Shetty, J.; Ward, T.; Herr, J.; Georg, G.
    Potent pyrimidine and pyrrolopyrimidine inhibitors of testis-specific serine/threonine kinase 2 (TSSK2) (2017), ChemMedChem, 12, 1857-1865 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.11.1

Inhibitors

Inhibitors Comment Organism Structure
1,1'-[(5-chloropyrimidine-2,4-diyl)bis[azanediyl(3-methoxy-4,1-phenylene)piperazine-4,1-diyl]]di(ethan-1-one)
-
 Homo sapiens
1-(6-[[4-(2,3-dihydro-1H-indol-1-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-5-methoxy-2,3-dihydro-1H-indol-1-yl)-2-(dimethylamino)ethan-1-one
-
 Homo sapiens
1-[3-methoxy-4-([6-[2-(propane-2-sulfonyl)anilino]-7H-purin-2-yl]amino)phenyl]piperidin-4-ol
-
 Homo sapiens
2,3-difluoro-6-[(2-[2-methoxy-4-[4-(propan-2-yl)piperazin-1-yl]anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]benzamide
-
 Homo sapiens
2-([5-bromo-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino)-N-methylbenzene-1-sulfonamide
-
 Homo sapiens
2-([5-chloro-2-[2-methoxy-4-(1-methylpiperidin-4-yl)anilino]pyrimidin-4-yl]amino)-N-methylbenzene-1-sulfonamide
-
 Homo sapiens
2-([5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino)-N-methylbenzene-1-sulfonamide
-
 Homo sapiens
2-([5-chloro-2-[2-methoxy-4-(morpholin-4-yl)anilino]pyrimidin-4-yl]amino)-N-methylbenzamide
-
 Homo sapiens
2-([5-chloro-2-[4-(piperazin-1-yl)anilino]pyrimidin-4-yl]amino)-N-methylbenzamide
-
 Homo sapiens
2-fluoro-6-([2-[(5-methoxy-1-[[4-(propan-2-yl)piperazin-1-yl]acetyl]-2,3-dihydro-1H-indol-6-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino)benzamide
-
 Homo sapiens
2-fluoro-6-[(2-[2-methoxy-4-[4-(propan-2-yl)piperazin-1-yl]anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]benzoic acid
-
 Homo sapiens
2-[(2-[4-chloro-2-methoxy-5-[(1-propylpiperidin-4-yl)oxy]anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-6-fluorobenzamide
-
 Homo sapiens
2-[(2-[5-[(N,N-dimethylglycyl)(methyl)amino]-2-methoxy-4-methylanilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-6-fluorobenzamide
-
 Homo sapiens
2-[(2-[5-[(N,N-dimethylglycyl)amino]-2-methoxy-4-methylanilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-6-fluorobenzamide
-
 Homo sapiens
2-[(2-[[1-(N,N-dimethylglycyl)-5-methoxy-2,3-dihydro-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-6-fluoro-N-methylbenzamide
-
 Homo sapiens
3-[(2-[[1-(N,N-dimethylglycyl)-6-methoxy-1,2,3,4-tetrahydroquinolin-7-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-N-methylpyridine-2-carboxamide
-
 Homo sapiens
3-[(2-[[1-(N,N-dimethylglycyl)-6-methoxy-1,2,3,4-tetrahydroquinolin-7-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]thiophene-2-carboxamide
-
 Homo sapiens
3-[(2-[[1-(N,N-dimethylglycyl)-6-methoxy-4,4-dimethyl-1,2,3,4-tetrahydroquinolin-7-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]thiophene-2-carboxamide
-
 Homo sapiens
4-fluoro-2-([2-[2-methoxy-4-(1-propylpiperidin-3-yl)anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino)benzamide
-
 Homo sapiens
4-fluoro-2-([2-[2-methoxy-4-(1-propylpiperidin-4-yl)anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino)benzamide
-
 Homo sapiens
5-chloro-N2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-N4-[2-(propane-2-sulfonyl)phenyl]pyrimidine-2,4-diamine
-
 Homo sapiens
5-chloro-N2-[4-[4-(dimethylamino)piperidin-1-yl]-2-methoxyphenyl]-N4-[2-(dimethylphosphoryl)phenyl]pyrimidine-2,4-diamine
-
 Homo sapiens
5-chloro-N2-[5-methyl-4-(piperidin-4-yl)-2-[(propan-2-yl)oxy]phenyl]-N4-[2-(propane-2-sulfonyl)phenyl]pyrimidine-2,4-diamine
-
 Homo sapiens
5-chloro-N4-[2-(dimethylphosphoryl)phenyl]-N2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]pyrimidine-2,4-diamine
-
 Homo sapiens
5-fluoro-2-[(2-[2-methoxy-4-[4-(propan-2-yl)piperazin-1-yl]anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]benzamide
-
 Homo sapiens
N-tert-butyl-3-([5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino)benzene-1-sulfonamide
-
 Homo sapiens
N-[(2R)-2,3-dihydroxypropyl]-5-fluoro-2-[(2-[2-methoxy-4-[4-(propan-2-yl)piperazin-1-yl]anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]benzamide
-
 Homo sapiens
N-[2-([5-chloro-2-[2-methoxy-4-(morpholin-4-yl)anilino]pyrimidin-4-yl]amino)phenyl]methanesulfonamide
-
 Homo sapiens
N-[2-([5-fluoro-2-[2-methoxy-4-(morpholin-4-yl)anilino]pyrimidin-4-yl]amino)phenyl]methanesulfonamide
-
 Homo sapiens
N-[3-([2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino)phenyl]prop-2-enamide
-
 Homo sapiens
N-[4-(4-aminopiperidin-1-yl)-2-methoxyphenyl]-5-chloro-4-(1H-indol-3-yl)pyrimidin-2-amine
-
 Homo sapiens
N2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-N4-[2-(propane-2-sulfonyl)phenyl]-1,3,5-triazine-2,4-diamine
-
 Homo sapiens
N2-[2-methoxy-4-[4-(propan-2-yl)piperazin-1-yl]phenyl]-N4-(quinolin-5-yl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q96PF2
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Synonyms

Synonyms Comment Organism
testis-specific serine/threonine kinase 2
-
 Homo sapiens
TSSK2
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000022
-
 pH and temperature not specified in the publication Homo sapiens 3-[(2-[[1-(N,N-dimethylglycyl)-6-methoxy-4,4-dimethyl-1,2,3,4-tetrahydroquinolin-7-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]thiophene-2-carboxamide
0.000031
-
 pH and temperature not specified in the publication Homo sapiens 2-([5-bromo-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino)-N-methylbenzene-1-sulfonamide
0.000037
-
 pH and temperature not specified in the publication Homo sapiens 2-([5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino)-N-methylbenzene-1-sulfonamide
0.000047
-
 pH and temperature not specified in the publication Homo sapiens 3-[(2-[[1-(N,N-dimethylglycyl)-6-methoxy-1,2,3,4-tetrahydroquinolin-7-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]thiophene-2-carboxamide
0.000058
-
 pH and temperature not specified in the publication Homo sapiens 1-[3-methoxy-4-([6-[2-(propane-2-sulfonyl)anilino]-7H-purin-2-yl]amino)phenyl]piperidin-4-ol
0.000066
-
 pH and temperature not specified in the publication Homo sapiens 2-([5-chloro-2-[2-methoxy-4-(1-methylpiperidin-4-yl)anilino]pyrimidin-4-yl]amino)-N-methylbenzene-1-sulfonamide
0.000072
-
 pH and temperature not specified in the publication Homo sapiens 5-fluoro-2-[(2-[2-methoxy-4-[4-(propan-2-yl)piperazin-1-yl]anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]benzamide
0.00008
-
 pH and temperature not specified in the publication Homo sapiens 5-chloro-N2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-N4-[2-(propane-2-sulfonyl)phenyl]pyrimidine-2,4-diamine
0.000107
-
 pH and temperature not specified in the publication Homo sapiens 4-fluoro-2-([2-[2-methoxy-4-(1-propylpiperidin-4-yl)anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino)benzamide
0.00015
-
 pH and temperature not specified in the publication Homo sapiens 2,3-difluoro-6-[(2-[2-methoxy-4-[4-(propan-2-yl)piperazin-1-yl]anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]benzamide
0.00023
-
 pH and temperature not specified in the publication Homo sapiens 5-chloro-N2-[4-[4-(dimethylamino)piperidin-1-yl]-2-methoxyphenyl]-N4-[2-(dimethylphosphoryl)phenyl]pyrimidine-2,4-diamine
0.000247
-
 pH and temperature not specified in the publication Homo sapiens 3-[(2-[[1-(N,N-dimethylglycyl)-6-methoxy-1,2,3,4-tetrahydroquinolin-7-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-N-methylpyridine-2-carboxamide
0.00025
-
 pH and temperature not specified in the publication Homo sapiens 4-fluoro-2-([2-[2-methoxy-4-(1-propylpiperidin-3-yl)anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino)benzamide
0.00028
-
 pH and temperature not specified in the publication Homo sapiens 2-[(2-[5-[(N,N-dimethylglycyl)amino]-2-methoxy-4-methylanilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-6-fluorobenzamide
0.00051
-
 pH and temperature not specified in the publication Homo sapiens 5-chloro-N4-[2-(dimethylphosphoryl)phenyl]-N2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]pyrimidine-2,4-diamine
0.00061
-
 pH and temperature not specified in the publication Homo sapiens 5-chloro-N2-[5-methyl-4-(piperidin-4-yl)-2-[(propan-2-yl)oxy]phenyl]-N4-[2-(propane-2-sulfonyl)phenyl]pyrimidine-2,4-diamine
0.00069
-
 pH and temperature not specified in the publication Homo sapiens N-[4-(4-aminopiperidin-1-yl)-2-methoxyphenyl]-5-chloro-4-(1H-indol-3-yl)pyrimidin-2-amine
0.00075
-
 pH and temperature not specified in the publication Homo sapiens N-[2-([5-chloro-2-[2-methoxy-4-(morpholin-4-yl)anilino]pyrimidin-4-yl]amino)phenyl]methanesulfonamide
0.000963
-
 pH and temperature not specified in the publication Homo sapiens 2-([5-chloro-2-[4-(piperazin-1-yl)anilino]pyrimidin-4-yl]amino)-N-methylbenzamide
0.0012
-
 pH and temperature not specified in the publication Homo sapiens N-[(2R)-2,3-dihydroxypropyl]-5-fluoro-2-[(2-[2-methoxy-4-[4-(propan-2-yl)piperazin-1-yl]anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]benzamide
0.0013
-
 pH and temperature not specified in the publication Homo sapiens 2-[(2-[4-chloro-2-methoxy-5-[(1-propylpiperidin-4-yl)oxy]anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-6-fluorobenzamide
0.0013
-
 pH and temperature not specified in the publication Homo sapiens 2-[(2-[[1-(N,N-dimethylglycyl)-5-methoxy-2,3-dihydro-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-6-fluoro-N-methylbenzamide
0.0015
-
 pH and temperature not specified in the publication Homo sapiens N2-[2-methoxy-4-[4-(propan-2-yl)piperazin-1-yl]phenyl]-N4-(quinolin-5-yl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.0021
-
 pH and temperature not specified in the publication Homo sapiens 2-fluoro-6-[(2-[2-methoxy-4-[4-(propan-2-yl)piperazin-1-yl]anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]benzoic acid
0.0038
-
 pH and temperature not specified in the publication Homo sapiens N2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-N4-[2-(propane-2-sulfonyl)phenyl]-1,3,5-triazine-2,4-diamine
0.0048
-
 pH and temperature not specified in the publication Homo sapiens 1-(6-[[4-(2,3-dihydro-1H-indol-1-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-5-methoxy-2,3-dihydro-1H-indol-1-yl)-2-(dimethylamino)ethan-1-one
0.006
-
 pH and temperature not specified in the publication Homo sapiens 2-fluoro-6-([2-[(5-methoxy-1-[[4-(propan-2-yl)piperazin-1-yl]acetyl]-2,3-dihydro-1H-indol-6-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino)benzamide
0.0062
-
 pH and temperature not specified in the publication Homo sapiens N-tert-butyl-3-([5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino)benzene-1-sulfonamide
0.0076
-
 pH and temperature not specified in the publication Homo sapiens 2-([5-chloro-2-[2-methoxy-4-(morpholin-4-yl)anilino]pyrimidin-4-yl]amino)-N-methylbenzamide
0.013
-
 pH and temperature not specified in the publication Homo sapiens N-[2-([5-fluoro-2-[2-methoxy-4-(morpholin-4-yl)anilino]pyrimidin-4-yl]amino)phenyl]methanesulfonamide
0.014
-
 pH and temperature not specified in the publication Homo sapiens 2-[(2-[5-[(N,N-dimethylglycyl)(methyl)amino]-2-methoxy-4-methylanilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-6-fluorobenzamide
0.015
-
 pH and temperature not specified in the publication Homo sapiens N-[3-([2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino)phenyl]prop-2-enamide
0.062
-
 pH and temperature not specified in the publication Homo sapiens 1,1'-[(5-chloropyrimidine-2,4-diyl)bis[azanediyl(3-methoxy-4,1-phenylene)piperazine-4,1-diyl]]di(ethan-1-one)

General Information

General Information Comment Organism
drug target the enzyme is an important target for reversible male contraception Homo sapiens