AZ628 [Ligand Id: 8475] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL2144069 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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 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 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 33:
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]
