BDBM454542 US10717746, Example 25::US10717746, Example 84
SMILES CC(=O)N[C@@H]1CCC[C@@H](C1)C(=O)Nc1cc(-c2cnn3CC(C)(C)Cc23)c(F)cn1
InChI Key InChIKey=JTIFUJUJDWUQEV-LSDHHAIUSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 18 hits for monomerid = 454542
Affinity DataIC50: <3nMAssay Description:Activity of CDK9 was determined in-vitro using a mobility shift assay on a Caliper LC3000 reader (Caliper/PerkinElmer), which measures fluorescence o...More data for this Ligand-Target Pair
Affinity DataEC50: 29nMAssay Description:Inhibition of CDK9 in human MV4-11 cells assessed as induction of caspase-3/7 activation measured after 6 hrs followed by Caspase-glo reagent based a...More data for this Ligand-Target Pair
Affinity DataIC50: 28nMAssay Description:Activity of CDK9 was determined in-vitro using a mobility shift assay on a Caliper LC3000 reader (Caliper/PerkinElmer), which measures fluorescence o...More data for this Ligand-Target Pair
Affinity DataIC50: 2.13E+3nMAssay Description:Activity of CDK9 was determined in-vitro using a mobility shift assay on a Caliper LC3000 reader (Caliper/PerkinElmer), which measures fluorescence o...More data for this Ligand-Target Pair
Affinity DataIC50: >3.00E+3nMAssay Description:Reversible inhibition of CDK9 in human MCF7 cells assessed as reduction in RNA Polymerase 2 CTD phosphorylation at Ser2 residues preincubated for 6 h...More data for this Ligand-Target Pair
Affinity DataKd: 569nMAssay Description:Binding affinity to human CDK9/CyclinT assessed as dissociation rate constant by surface plasmon resonance analysisMore data for this Ligand-Target Pair
Affinity DataKd: 0.123nMAssay Description:Binding affinity to human CDK9/CyclinT assessed as equilibrium dissociation constant by surface plasmon resonance analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 9.85E+3nMAssay Description:Inhibition of human recombinant N-terminal GST-TEV tagged CDK12 (696 to 1082 residues)/full length human CyclinK expressed in baculovirus expression ...More data for this Ligand-Target Pair
TargetCDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7(Homo sapiens (Human))
Astrazeneca
Curated by ChEMBL
Astrazeneca
Curated by ChEMBL
Affinity DataIC50: 548nMAssay Description:Inhibition of recombinant full length human CDK7/cyclinH1/MAT1 expressed in insect cells using 5FAM-YSPTSPSYSPTSPSYSPTSPSKKKK-NH2 as substrate preinc...More data for this Ligand-Target Pair
Affinity DataIC50: 532nMAssay Description:Inhibition of CDK6 (unknown origin) in presence of 5 mM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 2.78E+3nMAssay Description:Inhibition of CDK5 (unknown origin) in presence of 5 mM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 334nMAssay Description:Inhibition of CDK4 (unknown origin) in presence of 5 mM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Inhibition of CDK3 (unknown origin) in presence of 5 mM ATPMore data for this Ligand-Target Pair
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
Astrazeneca
Curated by ChEMBL
Astrazeneca
Curated by ChEMBL
Affinity DataIC50: 66nMAssay Description:Inhibition of recombinant full length human CDK2/CyclinE expressed in insect cells using FL-Ahx-QSPKKG-CONH2 as substrate preincubated for 10 mins fo...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase/G2/mitotic-specific cyclin- 1(Homo sapiens (Human))
Astrazeneca
Curated by ChEMBL
Astrazeneca
Curated by ChEMBL
Affinity DataIC50: 95nMAssay Description:Inhibition of recombinant full length human His-tagged CDK1/CyclinB expressed in baculovirus infected insect cells using 5FAM-RRRFRPASPLRGPPKCOOH as ...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of recombinant full length human N-terminal GST-fused CDK9 (1 to 372 residues)/His-tagged CyclinT1 (1 to 726 residues) expressed in baculo...More data for this Ligand-Target Pair
Affinity DataIC50: 25nMAssay Description:Inhibition of CDK9 in human MCF7 cells assessed as reduction in RNA Polymerase 2 CTD phosphorylation at Ser2 residues measured after 6 hrs by immunof...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Activity of CDK9 was determined in-vitro using a mobility shift assay on a Caliper LC3000 reader (Caliper/PerkinElmer), which measures fluorescence o...More data for this Ligand-Target Pair