AZ628 [Ligand Id: 8475] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2144069 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Heat shock factor protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5869] [UniProtKB: Q00613] | ||||||||
| ChEMBL | Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addition measured after 18 hrs by ELISA | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 180-201 [PMID:28004573] |
| ChEMBL | Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addition measured after 18 hrs by ELISA | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 180-201 [PMID:28004573] |
| Pirin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010627] [UniProtKB: O00625] | ||||||||
| ChEMBL | Displacement of 6-amino-9-(2-((4-((2-((6-((5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-methylphenyl)carbamoyl)quinolin-2-yl)oxy)ethyl)amino)-4-oxobutyl)(methyl)carbamoyl)phenyl)-3-imino-3H-xanthene-4,5-disulfonic acid from pirin (unknown origin) by fluorescence polarization assay | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2018) 9: 1199-1204 [PMID:30613326] |
| B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056] | ||||||||
| ChEMBL | Inhibition of human recombinant N-terminus His-tagged BRAF expressed in Sf9 cells coexpressing CDC37 using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 5 mM ATP | B | 5.58 | pIC50 | 2640 | nM | IC50 | J Med Chem (2013) 56: 1996-2015 [PMID:23398453] |
| ChEMBL | Inhibition of human recombinant N-terminus His-tagged BRAF V600E mutant expressed in Sf9 cells coexpressing CDC37 using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 5 mM ATP | B | 6.57 | pIC50 | 270 | nM | IC50 | J Med Chem (2013) 56: 1996-2015 [PMID:23398453] |
| ChEMBL | Inhibition of wild type B-Raf (unknown origin) | B | 6.98 | pIC50 | 105 | nM | IC50 | Eur J Med Chem (2020) 206: 112675-112675 [PMID:32798788] |
| ChEMBL | Inhibition of human recombinant N-terminus His-tagged BRAF V600E mutant expressed in Sf9 cells coexpressing CDC37 using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 10 uM ATP | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2013) 56: 1996-2015 [PMID:23398453] |
| ChEMBL | Inhibition of B-Raf V600E mutant (unknown origin) | B | 7.47 | pIC50 | 34 | nM | IC50 | Eur J Med Chem (2020) 206: 112675-112675 [PMID:32798788] |
| ChEMBL | Inhibition of B-Raf V600E mutant in human Malme-3M cells assessed as basal ERK phosphorylation | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 1923-1927 [PMID:24675381] |
| ChEMBL | Inhibition of BRAF V600E mutant-mediated ERK phosphorylation in human A375 cells after 75 mins | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2013) 56: 1996-2015 [PMID:23398453] |
| ChEMBL | Inhibition of recombinant human GST-tagged BRAF V600E mutant expressed in baculovirus expression system | B | 9 | pIC50 | <1 | nM | IC50 | ACS Med Chem Lett (2018) 9: 1199-1204 [PMID:30613326] |
| ChEMBL | Inhibition of wild type B-RAF (unknown origin) expressed in Escherichia coli BL21 (DE3) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2023) 250: 115231-115231 [PMID:36878151] |
| ChEMBL | Inhibition of B-RAF V600E mutant (unknown origin) expressed in Escherichia coli BL21 (DE3) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2023) 250: 115231-115231 [PMID:36878151] |
| ChEMBL | Inhibition of full-length B-Raf V600E mutant (unknown origin) | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 1923-1927 [PMID:24675381] |
| Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049] | ||||||||
| ChEMBL | Inhibition of wild type CRAF (unknown origin) using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 5 mM ATP | B | 6.42 | pIC50 | 380 | nM | IC50 | J Med Chem (2013) 56: 1996-2015 [PMID:23398453] |
| YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase YES in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947] | ||||||||
| ChEMBL | Inhibition of Yes1 (unknown origin) assessed as kinase-dependent enzymatic production of ADP from ATP using coupled luminescence-based reaction by ADP-Glo kinase assay | B | 6.46 | pIC50 | 348.3 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4398-4403 [PMID:23787099] |
| ChEMBL | Inhibition of Yes1 (unknown origin) by [gamma-33P]-ATP radiolabeled enzyme activity assay | B | 7.29 | pIC50 | 51.2 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4398-4403 [PMID:23787099] |
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]
