IPN60090 [Ligand Id: 12712] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4741924 (IACS-6274, Ipn 60090, Ipn-60090, IPN60090) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| glutaminase/Glutaminase kidney isoform, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2146302] [GtoPdb: 2891] [UniProtKB: O94925] | ||||||||
| ChEMBL | Inhibition of recombinant human GLS1 using glutamine as substrate preincubated for 10 mins followed by substrate addition and measured after 20 mins by glutamate oxidase/horseradish peroxidase-coupled Amplex UltraRED reagent based fluorescence assay | B | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2020) 63: 12957-12977 [PMID:33118821] |
| GtoPdb | - | - | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2020) 63: 12957-12977 [PMID:33118821] |
| ChEMBL | Inhibition of GLS1 in human A549 cells assessed as reduction in conversion of glutamine to glutamate measured after 24 hrs | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2020) 63: 12957-12977 [PMID:33118821] |
| Glutaminase liver isoform, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105730] [UniProtKB: Q9UI32] | ||||||||
| ChEMBL | Inhibition of recombinant human GLS2 using glutamine as substrate preincubated for 10 mins followed by substrate addition and measured for 20 mins by glutamate oxidase/horseradish peroxidase-coupled Amplex UltraRED reagent based fluorescence assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2020) 63: 12957-12977 [PMID:33118821] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG stably expressed in CHO cells at -80 mV by automated Qpatch electrophysiological assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2020) 63: 12957-12977 [PMID:33118821] |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Binding affinity to wild-type human partial length JAK3 JH1 catalytic domain (I781 to S1124 residues) expressed in mammalian expression system by Kinomescan method relative to control | B | 4.52 | pKd | >30000 | nM | Kd | J Med Chem (2020) 63: 12957-12977 [PMID:33118821] |
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]
