Lck inhibitor [Ligand Id: 6003] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL47940 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Apical membrane antigen 1 in Plasmodium falciparum 3D7 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559647] [UniProtKB: Q7KQK5] | ||||||||
| ChEMBL | Binding affinity to recombinant His-tagged Plasmodium falciparum 3D7 AMA1 assessed as inhibition of interaction with biotin-tagged RON2 peptide after 30 mins by AlphaScreen assay | B | 4.68 | pIC50 | 21000 | nM | IC50 | Medchemcomm (2014) 5: 1500-1506 |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067, P06493, P14635, Q8WWL7] | ||||||||
| ChEMBL | Inhibition of CDC2/CyB | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of Epidermal growth factor receptor | B | 5.49 | pIC50 | 3200 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antimalarial activity against Plasmodium falciparum FVO schizont infected in RBC assessed as inhibition of merozoite invasion after 3 to 4 hrs by flow cytometric analysis | F | 4.52 | pIC50 | 30000 | nM | IC50 | Medchemcomm (2014) 5: 1500-1506 |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5.3 | pIC50 | 5011.87 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.5 | pIC50 | 3162.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5.6 | pIC50 | 2511.89 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
| ChEMBL | Covalent inhibition of N-terminal GST-fused human BTK (2-659(end) amino acids) expressed in baculovirus expression system using FITC-AHA-EEPLYWSFPAKKK-NH2 as substrate incubated for 90 mins by microfluidic off-Chip Mobility Shift Assay | B | 6.51 | pIC50 | 310 | nM | IC50 | J Med Chem (2019) 62: 7643-7655 [PMID:31368705] |
| C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240] | ||||||||
| ChEMBL | Inhibition of Csk tyrosine kinase | B | 5.29 | pIC50 | 5180 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2171-2174 [PMID:11012022] |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | Inhibition of Fyn protein kinase | B | 6.9 | pIC50 | 126 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2171-2174 [PMID:11012022] |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Inhibition of p56 Lck tyrosine kinase catalytic domain at 1 mM ATP | B | 5.97 | pIC50 | 1070 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| ChEMBL | Inhibition of human p56 Lck tyrosine kinase (lck64-509) | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1683-1686 [PMID:12039590] |
| ChEMBL | Inhibition of p56 Lck tyrosine kinase at 1 mM ATP | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| ChEMBL | Inhibition of p56 Lck tyrosine kinase catalytic domain at 5 uM ATP | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| ChEMBL | Inhibition of p56 Lck tyrosine kinase (catalytic domain) | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2171-2174 [PMID:11012022] |
| GtoPdb | - | - | 9 | pIC50 | <1 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2171-4 [PMID:11012022] |
| ChEMBL | Inhibition of p56 Lck tyrosine kinase at 5 uM ATP | B | 9 | pIC50 | <1 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| ChEMBL | Inhibitory activity against p56 Lck tyrosine kinase at a concentration of 5 uM ATP. | B | 9 | pIC50 | <1 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2171-2174 [PMID:11012022] |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Inhibition of Protein tyrosine kinase Lyn | B | 6.38 | pIC50 | 420 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2171-2174 [PMID:11012022] |
| SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Inhibition of Src protein tyrosine kinase | B | 6.25 | pIC50 | 560 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1683-1686 [PMID:12039590] |
| ChEMBL | Inhibition of src at 5 mM ATP | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
| ChEMBL | Inhibition of TIE-2 kinase | B | 5.04 | pIC50 | 9070 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1683-1686 [PMID:12039590] |
| ChEMBL | Inhibition of tie-2 at 5 uM ATP | B | 5.7 | pIC50 | 1980 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| ChEMBL | Inhibitory activity against tie-2 at a concentration of 5 uM ATP. | B | 5.7 | pIC50 | 1980 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2171-2174 [PMID:11012022] |
| zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403] | ||||||||
| ChEMBL | Inhibition of Zap 70 | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Inhibition of Vascular endothelial growth factor receptor 2 | B | 5.35 | pIC50 | 4440 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1683-1686 [PMID:12039590] |
| ChEMBL | Inhibition of Vascular endothelial growth factor receptor 2 at 5 uM ATP | B | 5.8 | pIC50 | 1570 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| ChEMBL | Inhibitory activity against vascular endothelial growth factor receptor 2 (VEGFR2) at a concentration of 5 uM ATP. | B | 5.8 | pIC50 | 1570 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2171-2174 [PMID:11012022] |
ChEMBL data shown on this page come from version 32:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
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