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Literature summary for 2.7.10.2 extracted from

  • Zou, Y.; Xiao, J.; Tu, Z.; Zhang, Y.; Yao, K.; Luo, M.; Ding, K.; Zhang, Y.; Lai, Y.
    Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Brutons tyrosine kinase inhibitors (2016), Bioorg. Med. Chem. Lett., 26, 3052-3059 .
    View publication on PubMed
Search for more literature for 2.7.10.2

Inhibitors

Inhibitors Comment Organism Structure
1-(4-[5-(4-ethoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]piperazin-1-yl)prop-2-en-1-one inhibitory rate at 0.01 mM is 24.04% Homo sapiens
1-(4-[5-(4-phenoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]piperazin-1-yl)prop-2-en-1-one inhibitory rate at 0.01 mM is 48.54% Homo sapiens
1-(4-[[5-(4-ethoxybenzoyl)-6-(ethylamino)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one inhibitory rate at 0.01 mM is 6.81% Homo sapiens
1-(4-[[5-(4-ethoxybenzoyl)-6-(methylamino)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one inhibitory rate at 0.01 mM is % Homo sapiens
1-(4-[[6-(dimethylamino)-5-(4-ethoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one inhibitory rate at 0.01 mM is 9.8% Homo sapiens
1-(4-[[6-(ethylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one inhibitory rate at 0.01 mM is % Homo sapiens
1-(4-[[6-(methylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one inhibitory rate at 0.01 mM is 10.61% Homo sapiens
1-(4-[[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one inhibitory rate at 0.01 mM is 78.13% Homo sapiens
1-[(3R)-3-([5-(4-phenoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]amino)piperidin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 14.56% Homo sapiens
1-[(3R)-3-[[5-(4-ethoxybenzoyl)-6-(methylamino)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 10.27% Homo sapiens
1-[(3R)-3-[[5-(4-phenoxybenzoyl)-6-(piperidin-1-yl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 15.67% Homo sapiens
1-[(3R)-3-[[6-(dimethylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 11.42% Homo sapiens
1-[(3R)-3-[[6-(ethylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 18.24% Homo sapiens
1-[(3R)-3-[[6-(methylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 6.66% Homo sapiens
1-[(3R)-3-[[6-amino-5-(4-ethoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 52.88% Homo sapiens
1-[(3R)-3-[[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 100% Homo sapiens
1-[4-([5-(4-ethoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]amino)piperidin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 8.69% Homo sapiens
1-[4-([5-(4-phenoxybenzoyl)-6-[(propan-2-yl)amino]pyrimidin-4-yl]amino)piperidin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 1.2% Homo sapiens
1-[4-[5-(4-ethoxybenzoyl)-6-(ethylamino)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 6.43% Homo sapiens
1-[4-[5-(4-ethoxybenzoyl)-6-(methylamino)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 11-87% Homo sapiens
1-[4-[6-(ethylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 17.53% Homo sapiens
1-[4-[6-(methylamino)-5-(4-phenoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 8.14% Homo sapiens
1-[4-[6-amino-5-(4-ethoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 87.67 % Homo sapiens
1-[4-[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one inhibitory rate at 0.01 mM is 93.21% Homo sapiens
ibrutinib
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q06187
-
-

Synonyms

Synonyms Comment Organism
Bruton's tyrosine kinase
-
 Homo sapiens
Btk
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000065
-
 pH and temperature not specified in the publication Homo sapiens ibrutinib
0.00088
-
 pH and temperature not specified in the publication Homo sapiens 1-[4-[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
0.00107
-
 pH and temperature not specified in the publication Homo sapiens 1-(4-[[6-amino-5-(4-phenoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl)prop-2-en-1-one
0.00132
-
 pH and temperature not specified in the publication Homo sapiens 1-[4-[6-amino-5-(4-ethoxybenzoyl)pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
0.0018
-
 pH and temperature not specified in the publication Homo sapiens 1-[(3R)-3-[[6-amino-5-(4-ethoxybenzoyl)pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one

General Information

General Information Comment Organism
drug target the enzyme (BTK) is closely associated with the pathogenesis and development of various B-cell malignancies and autoimmune diseases, including rheumatoid arthritis, systemic lupus erythematosis, multiple sclerosis, B-cell lymphomas and leukemias, such as mantle cell lymphoma and chronic lymphocytic leukemia. Therefore, BTK has been considered as a potential therapeutic target for treating these diseases Homo sapiens
physiological function Bruton's tyrosine kinase plays a vital role in the B-cell signaling pathway linking cell surface B-cell receptor stimulation to downstream intracellular responses Homo sapiens