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 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]
