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Literature summary for 2.7.11.22 extracted from

  • Lee, J.; Choi, H.; Kim, K.H.; Jeong, S.; Park, J.W.; Baek, C.S.; Lee, S.H.
    Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors (2008), Bioorg. Med. Chem. Lett., 18, 2292-2295.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
2-(2-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
 Homo sapiens
2-(3-bromophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
 Homo sapiens
2-(3-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
 Homo sapiens
2-(4-aminophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
 Homo sapiens
2-(4-bromophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
 Homo sapiens
2-(4-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
 Homo sapiens
2-biphenyl-4-yl-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
 Homo sapiens
2-[4-(diethylamino)phenyl]-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
 Homo sapiens
2-[4-(dimethylamino)phenyl]-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
 Homo sapiens
N-(5-nitro-1H-indazol-3-yl)-2-phenylacetamide
-
 Homo sapiens
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(3-fluorophenyl)acetamide
-
 Homo sapiens
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(3-methylphenyl)acetamide
-
 Homo sapiens
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-fluorophenyl)acetamide
-
 Homo sapiens
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-hydroxyphenyl)acetamide
-
 Homo sapiens
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-methylphenyl)acetamide
-
 Homo sapiens
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-piperidin-1-ylphenyl)acetamide
-
 Homo sapiens
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-pyridin-4-ylphenyl)acetamide
-
 Homo sapiens
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-naphthalen-1-ylacetamide
-
 Homo sapiens
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-naphthalen-2-ylacetamide
-
 Homo sapiens
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-phenylacetamide
-
 Homo sapiens
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-[4-(methylsulfanyl)phenyl]acetamide
-
 Homo sapiens
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-[4-(methylsulfonyl)phenyl]acetamide
-
 Homo sapiens
N-[5-(2,5-dioxoimidazolidin-1-yl)-1H-indazol-3-yl]-2-phenylacetamide
-
 Homo sapiens
N-[5-(2-oxopiperidin-1-yl)-1H-indazol-3-yl]-2-phenylacetamide
-
 Homo sapiens
N-[5-(2-oxopyrrolidin-1-yl)-1H-indazol-3-yl]-2-phenylacetamide
-
 Homo sapiens
N-[5-(dibutylamino)-1H-indazol-3-yl]-2-phenylacetamide
-
 Homo sapiens
N-[5-(diethylamino)-1H-indazol-3-yl]-2-phenylacetamide
-
 Homo sapiens
N-[5-(dipropylamino)-1H-indazol-3-yl]-2-phenylacetamide
-
 Homo sapiens
N-[5-(ethylamino)-1H-indazol-3-yl]-2-phenylacetamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Homo sapiens P06493
-
-
Homo sapiens P24941
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
 Homo sapiens
-
EJ cell
-
 Homo sapiens
-
HCT-116 cell
-
 Homo sapiens
-
SW-620 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + histone H1
-
 Homo sapiens ADP + phosphorylated histone H1
-
 ?

Synonyms

Synonyms Comment Organism
Cdk1
-
 Homo sapiens
CDK2
-
 Homo sapiens
CDK4
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
cyclin
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000007
-
 with isozyme CDK2 Homo sapiens 2-(3-bromophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.000007
-
 with isozyme CDK2 Homo sapiens 2-(4-bromophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.000007
-
 with isozyme CDK2 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-methylphenyl)acetamide
0.000009
-
 with isozyme CDK2 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-hydroxyphenyl)acetamide
0.000009
-
 with isozyme CDK2 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-naphthalen-2-ylacetamide
0.00001
-
 with isozyme CDK2 Homo sapiens 2-[4-(dimethylamino)phenyl]-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.00001
-
 with isozyme CDK2 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(3-methylphenyl)acetamide
0.00001
-
 with isozyme CDK2 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-[4-(methylsulfanyl)phenyl]acetamide
0.000012
-
 with isozyme CDK1 Homo sapiens 2-(4-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.000012
-
 with isozyme CDK2 Homo sapiens 2-(4-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.000014
-
 with isozyme CDK2 Homo sapiens 2-biphenyl-4-yl-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.000016
-
 with isozyme CDK2 Homo sapiens 2-(4-aminophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.00002
-
 with isozyme CDK2 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-naphthalen-1-ylacetamide
0.000022
-
 with isozyme CDK1 Homo sapiens 2-(4-bromophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.000022
-
 with isozyme CDK2 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-[4-(methylsulfonyl)phenyl]acetamide
0.000028
-
 with isozyme CDK1 Homo sapiens 2-[4-(dimethylamino)phenyl]-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.000028
-
 with isozyme CDK1 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-hydroxyphenyl)acetamide
0.00003
-
 with isozyme CDK1 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(3-fluorophenyl)acetamide
0.00003
-
 with isozyme CDK2 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(3-fluorophenyl)acetamide
0.00003
-
 with isozyme CDK2 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-piperidin-1-ylphenyl)acetamide
0.00003
-
 with isozyme CDK2 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-pyridin-4-ylphenyl)acetamide
0.000034
-
 with isozyme CDK1 Homo sapiens 2-(3-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.000034
-
 with isozyme CDK2 Homo sapiens 2-(3-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.000036
-
 with isozyme CDK2 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-phenylacetamide
0.00004
-
 with isozyme CDK1 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-methylphenyl)acetamide
0.00004
-
 with isozyme CDK1 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-[4-(methylsulfanyl)phenyl]acetamide
0.00004
-
 with isozyme CDK1 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-naphthalen-2-ylacetamide
0.00004
-
 with isozyme CDK2 Homo sapiens 2-[4-(diethylamino)phenyl]-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.000042
-
 with isozyme CDK1 Homo sapiens 2-biphenyl-4-yl-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.000047
-
 with isozyme CDK1 Homo sapiens 2-(3-bromophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.00005
-
 with isozyme CDK1 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(3-methylphenyl)acetamide
0.00005
-
 with isozyme CDK1 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-fluorophenyl)acetamide
0.00005
-
 with isozyme CDK2 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-fluorophenyl)acetamide
0.00006
-
 with isozyme CDK1 Homo sapiens 2-[4-(diethylamino)phenyl]-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.00006
-
 with isozyme CDK1 Homo sapiens 2-(4-aminophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.00006
-
 with isozyme CDK1 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-pyridin-4-ylphenyl)acetamide
0.000067
-
 with isozyme CDK1 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-naphthalen-1-ylacetamide
0.00008
-
 with isozyme CDK1 Homo sapiens 2-(2-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.00008
-
 with isozyme CDK1 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-phenylacetamide
0.00008
-
 with isozyme CDK2 Homo sapiens 2-(2-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.00015
-
 with isozyme CDK1 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-piperidin-1-ylphenyl)acetamide
0.00017
-
 with isozyme CDK2 Homo sapiens N-[5-(2-oxopyrrolidin-1-yl)-1H-indazol-3-yl]-2-phenylacetamide
0.0002
-
 with isozyme CDK1 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-[4-(methylsulfonyl)phenyl]acetamide
0.0002
-
 with isozyme CDK2 Homo sapiens N-[5-(diethylamino)-1H-indazol-3-yl]-2-phenylacetamide
0.00021
-
 with isozyme CDK4 Homo sapiens 2-[4-(dimethylamino)phenyl]-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.0005
-
 with isozyme CDK2 Homo sapiens N-[5-(ethylamino)-1H-indazol-3-yl]-2-phenylacetamide
0.00071
-
 with isozyme CDK4 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(3-fluorophenyl)acetamide
0.00075
-
 with isozyme CDK4 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-piperidin-1-ylphenyl)acetamide
0.00089
-
 with isozyme CDK4 Homo sapiens 2-(2-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.001
-
 with isozyme CDK4, IC50 above 0.001 mM Homo sapiens 2-[4-(diethylamino)phenyl]-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.00105
-
 with isozyme CDK4 Homo sapiens 2-(3-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.0013
-
 with isozyme CDK4 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-[4-(methylsulfanyl)phenyl]acetamide
0.00133
-
 with isozyme CDK4 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-pyridin-4-ylphenyl)acetamide
0.0014
-
 with isozyme CDK4 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-[4-(methylsulfonyl)phenyl]acetamide
0.0016
-
 with isozyme CDK4 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-naphthalen-2-ylacetamide
0.00175
-
 with isozyme CDK4 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-hydroxyphenyl)acetamide
0.0018
-
 with isozyme CDK2 Homo sapiens N-[5-(dipropylamino)-1H-indazol-3-yl]-2-phenylacetamide
0.0018
-
 with isozyme CDK4 Homo sapiens 2-(3-bromophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.0018
-
 with isozyme CDK4 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-methylphenyl)acetamide
0.002
-
 with isozyme CDK2 Homo sapiens N-(5-nitro-1H-indazol-3-yl)-2-phenylacetamide
0.002
-
 with isozyme CDK2 Homo sapiens N-[5-(2,5-dioxoimidazolidin-1-yl)-1H-indazol-3-yl]-2-phenylacetamide
0.002
-
 with isozyme CDK4 Homo sapiens 2-(4-bromophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.002
-
 with isozyme CDK4 Homo sapiens 2-(4-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.0022
-
 with isozyme CDK4 Homo sapiens 2-biphenyl-4-yl-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.0022
-
 with isozyme CDK4 Homo sapiens 2-(4-aminophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
0.003
-
 with isozyme CDK4 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-naphthalen-1-ylacetamide
0.003
-
 with isozyme CDK4 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-fluorophenyl)acetamide
0.0037
-
 with isozyme CDK4 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-phenylacetamide
0.004
-
 with isozyme CDK4 Homo sapiens N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(3-methylphenyl)acetamide
0.0071
-
 with isozyme CDK2 Homo sapiens N-[5-(2-oxopiperidin-1-yl)-1H-indazol-3-yl]-2-phenylacetamide
0.1
-
 with isozyme CDK2, IC50 above 0.1 mM Homo sapiens N-[5-(dibutylamino)-1H-indazol-3-yl]-2-phenylacetamide