BDBM50528817 CHEMBL4462530::US10717746, Example 14::US20230416221, Compound AZD4573
SMILES CC(=O)N[C@@H]1CCC[C@@H](C1)C(=O)Nc1cc(-c2cnn3CC(C)(C)Cc23)c(Cl)cn1
InChI Key InChIKey=AVIWDYSJSPOOAR-LSDHHAIUSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 31 hits for monomerid = 50528817
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
3D Structure (crystal)TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
Affinity DataIC50: 13nMAssay Description:The DMSO diluted compounds and the control compounds Dinaciclib, JSH-009, BAY-1211152, AZD4573 (all purchased from MCE, China) were mixed with the de...More data for this Ligand-Target Pair
Affinity DataIC50: <4nMAssay Description:Inhibition of CDK9 (unknown origin)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 DataIC50: 5.52E+3nMAssay Description:Inhibition of CK1gamma1 (unknown origin) in presence of 5 mM ATPMore data for this Ligand-Target Pair
TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
Affinity DataKd: 711nMAssay Description:Binding affinity to human CDK9/CyclinT assessed as dissociation rate constant by surface plasmon resonance analysisMore data for this Ligand-Target Pair
TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
Affinity DataKd: 0.0894nMAssay 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: 8.07E+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: 1.37E+3nMAssay 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: 363nMAssay Description:Inhibition of CDK6 (unknown origin) in presence of 5 mM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 1.27E+3nMAssay Description:Inhibition of CDK5 (unknown origin) in presence of 5 mM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 499nMAssay Description:Inhibition of CDK4 (unknown origin) in presence of 5 mM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 23nMAssay 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: 52nMAssay 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: 117nMAssay 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: 6.66E+3nMAssay Description:Inhibition of CK1gamma2 (unknown origin) in presence of 5 mM ATPMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 2(Homo sapiens (Human))
Astrazeneca
Curated by ChEMBL
Astrazeneca
Curated by ChEMBL
Affinity DataIC50: 8.62E+3nMAssay Description:Inhibition of DYRK2 (unknown origin) in presence of 5 mM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 187nMAssay Description:Inhibition of GSK3alpha (unknown origin) in presence of 5 mM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 247nMAssay Description:Inhibition of GSK3beta (unknown origin) in presence of 5 mM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 2.80E+3nMAssay Description:Inhibition of JNK1 (unknown origin) in presence of 5 mM ATPMore data for this Ligand-Target Pair
TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
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: 13nMAssay 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 DataEC50: 14nMAssay 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
TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
Affinity DataIC50: <4nMAssay Description:Inhibition of full length human CDK9 (1 to 372 residues)/His-tagged CyclinT1 (1 to 726 residues) expressed in baculovirus expression system in presen...More data for this Ligand-Target Pair
TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
Affinity DataIC50: <3nMAssay Description:Inhibition of full length human CDK9 (1 to 372 residues)/His-tagged CyclinT1 (1 to 726 residues) expressed in baculovirus expression system in presen...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 1(Homo sapiens (Human))
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 370nMAssay Description:Inhibition of CDK1 in human MCF7 cells assessed as reduction in PP1alpha phosphorylation at T320 residue incubated for 6 hrs by immunoblot analysisMore data for this Ligand-Target Pair
TargetCyclin-dependent kinase 2(Homo sapiens (Human))
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CDK2 in human MCF7 cells assessed as reduction in Rb phosphorylation at T821 residue incubated for 6 hrs by immunoblot analysisMore data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/6(Homo sapiens (Human))
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CDK4/6 in human MCF7 cells assessed as reduction in Rb phosphorylation at S807/811 residue incubated for 6 hrs by immunoblot analysisMore data for this Ligand-Target Pair
TargetCyclin-dependent kinase 7(Homo sapiens (Human))
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 1.10E+3nMAssay Description:Inhibition of CDK7 in human MCF7 cells assessed as RNA polymerase2 phosphorylation at serine 5 residue residue incubated for 6 hrs by immunoblot anal...More data for this Ligand-Target Pair
TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
Hefei Institutes Of Physical Science, Chinese Academy Of Sciences
US Patent
Affinity DataIC50: <4nMAssay Description:Inhibition of CDK9/Cyclin T (unknown origin) in presence of ATP by Kinomescan assayMore 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