compound 31 [PMID: 22902653] [Ligand Id: 8117] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2070615
  • testis associated actin remodelling kinase 1/Dual specificity testis-specific protein kinase 1 in Human [ChEMBL: CHEMBL5604] [GtoPdb: 2239] [UniProtKB: Q15569]
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  • testis associated actin remodelling kinase 2/Dual specificity testis-specific protein kinase 2 in Human [ChEMBL: CHEMBL2069163] [GtoPdb: 2240] [UniProtKB: Q96S53]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
testis associated actin remodelling kinase 1/Dual specificity testis-specific protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5604] [GtoPdb: 2239] [UniProtKB: Q15569]
GtoPdb - - 6.34 pIC50 455 nM IC50 Bioorg Med Chem Lett (2012) 22: 5995-8 [PMID:22902653]
ChEMBL Inhibition of TESK1 B 6.34 pIC50 455 nM IC50 Bioorg Med Chem Lett (2012) 22: 5995-5998 [PMID:22902653]
testis associated actin remodelling kinase 2/Dual specificity testis-specific protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069163] [GtoPdb: 2240] [UniProtKB: Q96S53]
ChEMBL Inhibition of TESK2 B 6.6 pIC50 252 nM IC50 Bioorg Med Chem Lett (2012) 22: 5995-5998 [PMID:22902653]
GtoPdb - - 6.6 pIC50 252 nM IC50 Bioorg Med Chem Lett (2012) 22: 5995-8 [PMID:22902653]
LIM domain kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3836] [GtoPdb: 2054] [UniProtKB: P53667]
ChEMBL Inhibition of PAK mediated recombinant LIMK1 phosphorylation (330 to 637 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 105 mins by RapidFire Mass Spectrometry kinase assay B 5.64 pIC50 2290.87 nM IC50 J Med Chem (2022) 65: 13705-13713 [PMID:36205722]
ChEMBL Inhibition of recombinant LIMK1(unknown origin) expressed in HEK293 cells using NanoGlo substrate incubated for 2 hrs followed by substrate addition by NanoBRET assay B 6.45 pIC50 354.81 nM IC50 J Med Chem (2022) 65: 13705-13713 [PMID:36205722]
ChEMBL Inhibition of human LIMK1 (321 to 647 residues) expressed in Sf9 cells using dextrin as substrate incubated for 30 mins by micro-scintillation fluid method B 7.24 pIC50 58 nM IC50 Eur J Med Chem (2018) 155: 445-458 [PMID:29908439]
ChEMBL Inhibition of LIMK1 B 7.24 pIC50 58 nM IC50 Bioorg Med Chem Lett (2012) 22: 5995-5998 [PMID:22902653]
GtoPdb - - 7.24 pIC50 58 nM IC50 Bioorg Med Chem Lett (2012) 22: 5995-8 [PMID:22902653]
ChEMBL Inhibition of recombinant LIMK1 (330 to 637 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 105 mins by RapidFire Mass Spectrometry kinase assay B 7.25 pIC50 56.23 nM IC50 J Med Chem (2022) 65: 13705-13713 [PMID:36205722]
ChEMBL Inhibition of LIMK1 (unknown origin) assessed as ADP formation using cofilin-2 protein as substrate measured after 60 mins incubation with enzyme by Transcreener assay B 7.27 pIC50 54 nM IC50 Medchemcomm (2011) 2: 982-986
ChEMBL Inhibition of LIMK1-catalyzed cofilin phosphorylation in human ZR-75-1 cells B 9 pIC50 1 nM IC50 Medchemcomm (2011) 2: 982-986
LIM domain kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5932] [GtoPdb: 2055] [UniProtKB: P53671]
ChEMBL Inhibition of PAK mediated recombinant LIMK2 phosphorylation (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay B 6.15 pIC50 707.95 nM IC50 J Med Chem (2022) 65: 13705-13713 [PMID:36205722]
ChEMBL Inhibition of LIMK2 (unknown origin) B 6.16 pIC50 696 nM IC50 Medchemcomm (2011) 2: 982-986
ChEMBL Inhibition of recombinant LIMK2(unknown origin) expressed in HEK293 cells using NanoGlo substrate incubated for 2 hrs followed by substrate addition by NanoBRET assay B 6.33 pIC50 467.74 nM IC50 J Med Chem (2022) 65: 13705-13713 [PMID:36205722]
ChEMBL Inhibition of recombinant LIMK2 (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay B 6.87 pIC50 134.9 nM IC50 J Med Chem (2022) 65: 13705-13713 [PMID:36205722]
GtoPdb - - 7.42 pIC50 38 nM IC50 Bioorg Med Chem Lett (2012) 22: 5995-8 [PMID:22902653]
ChEMBL Inhibition of LIMK2 B 7.42 pIC50 38 nM IC50 Bioorg Med Chem Lett (2012) 22: 5995-5998 [PMID:22902653]
ChEMBL Inhibition of human LIMK1 (312 to 638 residues) expressed in Sf9 cells using dextrin as substrate incubated for 30 mins by micro-scintillation fluid method B 7.42 pIC50 38 nM IC50 Eur J Med Chem (2018) 155: 445-458 [PMID:29908439]

ChEMBL data shown on this page come from version 34:

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]