Cdk2 inhibitor III [Ligand Id: 5948] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL80713
  • phosphodiesterase 4D/3`,5`-cyclic-AMP phosphodiesterase 4D in Human [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
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  • phosphodiesterase 10A/cAMP and cAMP-inhibited cGMP 3`,5`-cyclic phosphodiesterase 10A in Human [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233]
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  • phosphodiesterase 2A/cGMP-dependent 3`,5`-cyclic phosphodiesterase in Human [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
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  • phosphodiesterase 3A/cGMP-inhibited 3`,5`-cyclic phosphodiesterase 3A in Human [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432]
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  • phosphodiesterase 5A/cGMP-specific 3`,5`-cyclic phosphodiesterase in Human [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
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  • phosphodiesterase 11A/Dual 3`,5`-cyclic-AMP and -GMP phosphodiesterase 11A in Human [ChEMBL: CHEMBL2717] [GtoPdb: 1311] [UniProtKB: Q9HCR9]
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  • phosphodiesterase 1A/Dual specificity calcium/calmodulin-dependent 3`,5`-cyclic nucleotide phosphodiesterase 1A in Human [ChEMBL: CHEMBL3421] [GtoPdb: 1294] [UniProtKB: P54750]
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  • phosphodiesterase 7A/High affinity 3`,5`-cyclic-AMP phosphodiesterase 7A in Human [ChEMBL: CHEMBL3012] [GtoPdb: 1305] [UniProtKB: Q13946]
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  • phosphodiesterase 8A/High affinity cAMP-specific and IBMX-insensitive 3`,5`-cyclic phosphodiesterase 8A in Human [ChEMBL: CHEMBL4640] [GtoPdb: 1307] [UniProtKB: O60658]
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  • phosphodiesterase 9A/High affinity cGMP-specific 3`,5`-cyclic phosphodiesterase 9A in Human [ChEMBL: CHEMBL3535] [GtoPdb: 1309] [UniProtKB: O76083]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
phosphodiesterase 4D/3`,5`-cyclic-AMP phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
ChEMBL Inhibition of his-tagged recombinant human PDE4D catalytic domain (T86 to S413 residues) expressed in Escherichia coli BL21(DE3) using [3H]-cAMP as substrate incubated for 10 mins by SPA assay B 6.38 pIC50 420 nM IC50 Eur J Med Chem (2023) 262: 115893-115893 [PMID:37918035]
phosphodiesterase 10A/cAMP and cAMP-inhibited cGMP 3`,5`-cyclic phosphodiesterase 10A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233]
ChEMBL Inhibition of his-tagged recombinant human PDE10A catalytic domain (S439 to A766 residues) expressed in Escherichia coli BL21(DE3) using [3H]-cAMP as substrate incubated for 10 mins by SPA assay B 5.89 pIC50 1290 nM IC50 Eur J Med Chem (2023) 262: 115893-115893 [PMID:37918035]
cyclin dependent kinase 2/CDK2/Cyclin A2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941]
GtoPdb CDK2/cyclin E complex - 6.3 pIC50 500 nM IC50 Bioorg Med Chem Lett (1997) 7: 2697-2702
ChEMBL Inhibition of GST-tagged CDK2/cyclin A2 (unknown origin) expressed in Escherichia coli using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 6.66 pIC50 220 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 7/CDK7/Cyclin H/MNAT1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038473] [GtoPdb: 1979] [UniProtKB: P50613, P51946, P51948]
ChEMBL Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 5.04 pIC50 9200 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750]
ChEMBL Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 5.64 pIC50 2300 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
phosphodiesterase 2A/cGMP-dependent 3`,5`-cyclic phosphodiesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
ChEMBL Inhibition of full-length recombinant human PDE2A using [3H]-cGMP as substrate incubated for 10 mins by SPA assay B 6 pIC50 >1000 nM IC50 Eur J Med Chem (2023) 262: 115893-115893 [PMID:37918035]
phosphodiesterase 3A/cGMP-inhibited 3`,5`-cyclic phosphodiesterase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432]
ChEMBL Inhibition of full-length recombinant human PDE3A using [3H]-cGMP as substrate incubated for 10 mins by SPA assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2023) 262: 115893-115893 [PMID:37918035]
phosphodiesterase 5A/cGMP-specific 3`,5`-cyclic phosphodiesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
ChEMBL Inhibition of his-tagged recombinant human PDE5A catalytic domain (E535 to Q860 residues) expressed in Escherichia coli BL21(DE3) using [3H]-cGMP as substrate incubated for 10 mins by SPA assay B 6.64 pIC50 230 nM IC50 Eur J Med Chem (2023) 262: 115893-115893 [PMID:37918035]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635]
GtoPdb CDK1/cyclin B complex - 5.38 pIC50 4200 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
ChEMBL Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 5.43 pIC50 3700 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094126] [GtoPdb: 1973] [UniProtKB: O96020, P24864, P24941]
GtoPdb CDK2/cyclin E complex - 6.3 pIC50 500 nM IC50 Bioorg Med Chem Lett (1997) 7: 2697-2702
ChEMBL Inhibitory concentration against cyclin dependent kinase-2 (CDK2)/Cyclin E B 6.3 pIC50 500 nM IC50 Bioorg Med Chem Lett (1997) 7: 2697-2702
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941]
GtoPdb CDK2/cyclin E complex - 6.3 pIC50 500 nM IC50 Bioorg Med Chem Lett (1997) 7: 2697-2702
ChEMBL Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 6.75 pIC50 176 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385]
ChEMBL Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 4.7 pIC50 >20000 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
ChEMBL Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 6.38 pIC50 419 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
phosphodiesterase 11A/Dual 3`,5`-cyclic-AMP and -GMP phosphodiesterase 11A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2717] [GtoPdb: 1311] [UniProtKB: Q9HCR9]
ChEMBL Inhibition of full-length recombinant human PDE11A using [3H]-cAMP as substrate incubated for 10 mins by SPA assay B 6 pIC50 >1000 nM IC50 Eur J Med Chem (2023) 262: 115893-115893 [PMID:37918035]
phosphodiesterase 1A/Dual specificity calcium/calmodulin-dependent 3`,5`-cyclic nucleotide phosphodiesterase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3421] [GtoPdb: 1294] [UniProtKB: P54750]
ChEMBL Inhibition of full-length recombinant human PDE1A using [3H]-cGMP as substrate incubated for 10 mins by SPA assay B 6 pIC50 >1000 nM IC50 Eur J Med Chem (2023) 262: 115893-115893 [PMID:37918035]
phosphodiesterase 7A/High affinity 3`,5`-cyclic-AMP phosphodiesterase 7A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3012] [GtoPdb: 1305] [UniProtKB: Q13946]
ChEMBL Inhibition of his-tagged recombinant human PDE7A catalytic domain (S130 to S482 residues) expressed in Escherichia coli BL21(DE3) using [3H]-cAMP as substrate incubated for 10 mins by SPA assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2023) 262: 115893-115893 [PMID:37918035]
phosphodiesterase 8A/High affinity cAMP-specific and IBMX-insensitive 3`,5`-cyclic phosphodiesterase 8A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4640] [GtoPdb: 1307] [UniProtKB: O60658]
ChEMBL Inhibition of full-length recombinant human PDE8A using [3H]-cAMP as substrate incubated for 10 mins by SPA assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2023) 262: 115893-115893 [PMID:37918035]
phosphodiesterase 9A/High affinity cGMP-specific 3`,5`-cyclic phosphodiesterase 9A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3535] [GtoPdb: 1309] [UniProtKB: O76083]
ChEMBL Inhibition of his-tagged recombinant human PDE9A catalytic domain (P181 to K506 residues) expressed in Escherichia coli BL21(DE3) using [3H]-cGMP as substrate incubated for 10 mins by SPA assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2023) 262: 115893-115893 [PMID:37918035]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]