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ChEMBL ligand: CHEMBL225519 (PHA-767491) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] | ||||||||
ChEMBL | Inhibition of Alk | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612] | ||||||||
ChEMBL | Inhibition of PKAalpha | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
cell division cycle 7/Cell division cycle 7-related protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5443] [GtoPdb: 1960] [UniProtKB: O00311] | ||||||||
ChEMBL | Inhibition of human Cdc7 | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2008) 51: 487-501 [PMID:18201066] |
ChEMBL | Inhibition of human Cdc7 assessed as inhibition of rate of phosphorylation of Mcm2 protein | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2009) 52: 293-307 [PMID:19115845] |
ChEMBL | Inhibition of cdc7 | B | 8 | pIC50 | 10 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
ChEMBL | Inhibition of Cdc7 | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2010) 53: 7296-7315 [PMID:20873740] |
ChEMBL | Inhibition of Cdc7 (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
ChEMBL | Inhibition of CDC7 (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2021) 64: 1283-1345 [PMID:33481605] |
ChEMBL | Inhibition of human cdc7 incubation of 30 mins in presence of ATP | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2021) 64: 2382-2418 [PMID:33650861] |
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
ChEMBL | Inhibition of cdk1 | B | 6.6 | pIC50 | 250 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
ChEMBL | Inhibition of CDK2 | B | 6.77 | pIC50 | 170 | nM | IC50 | J Med Chem (2007) 50: 2647-2654 [PMID:17480064] |
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
ChEMBL | Inhibition of cdk2 | B | 6.62 | pIC50 | 240 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
ChEMBL | Inhibition of cdk5 | B | 6.34 | pIC50 | 460 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] | ||||||||
ChEMBL | Inhibition of Cdk7 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
ChEMBL | Inhibition of CDK9 | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2009) 52: 293-307 [PMID:19115845] |
ChEMBL | Inhibition of cdk9 | B | 7.47 | pIC50 | 34 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
ChEMBL | Inhibition of CDK9 (unknown origin) | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
ChEMBL | Inhibition of human CDK9 incubation of 30 mins in presence of ATP | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2021) 64: 2382-2418 [PMID:33650861] |
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
ChEMBL | Inhibition of FGFR1 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
ChEMBL | Inhibition of GSK3-beta | B | 6.66 | pIC50 | 220 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
ChEMBL | Inhibition of c-Met | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920] | ||||||||
ChEMBL | Inhibition of IKK2 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2007) 50: 2647-2654 [PMID:17480064] |
ChEMBL | Inhibition of IKK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
ChEMBL | Inhibition of IR | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137] | ||||||||
ChEMBL | Inhibition of Mk2 | B | 6.33 | pIC50 | 470 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
ChEMBL | Inhibition of MK2 | B | 6.77 | pIC50 | 171 | nM | IC50 | J Med Chem (2007) 50: 2647-2654 [PMID:17480064] |
GtoPdb | - | - | 6.77 | pIC50 | 171 | nM | IC50 | J Med Chem (2007) 50: 2647-54 [PMID:17480064] |
MAPK activated protein kinase 3/MAP kinase-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4670] [GtoPdb: 2095] [UniProtKB: Q16644] | ||||||||
ChEMBL | Inhibition of MK3 | B | 4.24 | pIC50 | 57700 | nM | IC50 | J Med Chem (2007) 50: 2647-2654 [PMID:17480064] |
MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41] | ||||||||
ChEMBL | Inhibition of MK5 | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2007) 50: 2647-2654 [PMID:17480064] |
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
ChEMBL | Inhibition of ERK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5] | ||||||||
ChEMBL | Inhibition of MNK1 | B | 5.57 | pIC50 | 2670 | nM | IC50 | J Med Chem (2007) 50: 2647-2654 [PMID:17480064] |
ChEMBL | Inhibition of MNK1 | B | 5.57 | pIC50 | 2670 | nM | IC50 | J Med Chem (2010) 53: 6618-6628 [PMID:20722422] |
mitogen-activated protein kinase 11/MAP kinase p38 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759] | ||||||||
ChEMBL | Inhibition of P38beta | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] | ||||||||
ChEMBL | Inhibition of MNK2 | B | 6.77 | pIC50 | 171 | nM | IC50 | J Med Chem (2010) 53: 6618-6628 [PMID:20722422] |
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
ChEMBL | Inhibition of TRKA | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771] | ||||||||
ChEMBL | Inhibition of PKCbeta | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
protein kinase N1/Protein kinase N1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512] | ||||||||
ChEMBL | Inhibition of PKN1 (unknown origin) by TR-FRET-based tracer displacement assay dependent Cheng-Prusoff equation analysis | B | 6.82 | pKi | 150 | nM | Ki | Bioorg Med Chem Lett (2022) 60: 128588-128588 [PMID:35104640] |
ChEMBL | Inhibition of PKN1 (unknown origin) by TR-FRET-based tracer displacement assay | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem Lett (2022) 60: 128588-128588 [PMID:35104640] |
protein kinase N2/Protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513] | ||||||||
ChEMBL | Inhibition of PKN2 (unknown origin) by TR-FRET-based tracer displacement assay dependent Cheng-Prusoff equation analysis | B | 8.1 | pKi | 8 | nM | Ki | Bioorg Med Chem Lett (2022) 60: 128588-128588 [PMID:35104640] |
ChEMBL | Inhibition of NanoLuc-PKN2 (ser646-cys984)(unknown origin) expressed in HEK293 cells by cell-based NanoBRET target engagement assay | B | 5.32 | pIC50 | 4800 | nM | IC50 | Bioorg Med Chem Lett (2022) 60: 128588-128588 [PMID:35104640] |
ChEMBL | Inhibition of PKN2 (unknown origin) by TR-FRET-based tracer displacement assay | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2022) 60: 128588-128588 [PMID:35104640] |
pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118] | ||||||||
ChEMBL | Inhibition of PDK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
ribosomal protein S6 kinase A4/Ribosomal protein S6 kinase alpha 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3125] [GtoPdb: 1524] [UniProtKB: O75676] | ||||||||
GtoPdb | - | - | 5.52 | pIC50 | 3010 | nM | IC50 | J Med Chem (2007) 50: 2647-54 [PMID:17480064] |
ChEMBL | Inhibition of MSK2 | B | 5.52 | pIC50 | 3010 | nM | IC50 | J Med Chem (2007) 50: 2647-2654 [PMID:17480064] |
ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582] | ||||||||
ChEMBL | Inhibition of MSK1 | B | 5.63 | pIC50 | 2340 | nM | IC50 | J Med Chem (2007) 50: 2647-2654 [PMID:17480064] |
STE20 like kinase/Serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2] | ||||||||
ChEMBL | Inhibition of STLK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
ChEMBL | Inhibition of AKT1 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
ChEMBL | Inhibition of Aurora-A | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] | ||||||||
ChEMBL | Inhibition of Aurora-B | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
ChEMBL | Inhibition of chk1 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017] | ||||||||
ChEMBL | Inhibition of chk2 | B | 5.96 | pIC50 | 1100 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
NIMA related kinase 6/Serine/threonine-protein kinase NEK6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98] | ||||||||
ChEMBL | Inhibition of Nek6 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
serine/threonine-protein kinase NIM1/Serine/threonine-protein kinase NIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3542] [GtoPdb: 2291] [UniProtKB: Q8IY84] | ||||||||
ChEMBL | Inhibition of NIM1 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013] | ||||||||
ChEMBL | Inhibition of PAK4 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
ChEMBL | Inhibition of plk1 | B | 6.01 | pIC50 | 980 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8] | ||||||||
ChEMBL | Inhibition of TAO3 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
ChEMBL | Inhibition of c-Kit | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
ChEMBL | Inhibition of c-Abl | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
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 LCK | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
ChEMBL | Inhibition of Ret | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
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 ZAP70 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
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 VEGFR2 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
ChEMBL | Inhibition of VEGFR3 | B | 5 | pIC50 | >10000 | nM | IC50 | Nat Chem Biol (2008) 4: 357-365 [PMID:18469809] |
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]