pevonedistat [Ligand Id: 12117] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1231160 (MLN 4924, MLN-4924, MLN4924, MLN-4924003, Pevonedistat) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| NEDD8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295831] [UniProtKB: Q15843] | ||||||||
| ChEMBL | Inhibition of NEDD8 (unknown origin) assessed as decrease in formation of E2-UBL thioester reaction product | B | 8.33 | pIC50 | 4.7 | nM | IC50 | J Med Chem (2018) 61: 3239-3252 [PMID:28505447] |
| NEDD8 activating enzyme in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3831283] [UniProtKB: Q13564, Q8TBC4] | ||||||||
| ChEMBL | Inhibition of NAE1/UBA3 in human HCT-116 cells assessed as reduction in Ubc12-NEDD8 level incubated for 24 hrs by immunoblot analysis | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2022) 231: 114156-114156 [PMID:35131538] |
| ChEMBL | Inhibition of NAE (unknown origin) | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2021) 64: 6161-6178 [PMID:33857374] |
| ChEMBL | Inhibition of NAE (unknown origin) mediated neddylation assessed as decrease in NEDD8-Ubcl2 adduct formation incubated for 2 hrs in presence of L-glutathione and ATP by HTRF assay | B | 9.59 | pIC50 | 0.26 | nM | IC50 | J Med Chem (2021) 64: 6161-6178 [PMID:33857374] |
| ChEMBL | Inhibition of NAE-mediated Ubcl2-NEDD8 conjugation in human Caco2 cells after 16 hrs by Western blot analysis | B | 5.47 | pEC50 | 3400 | nM | EC50 | Eur J Med Chem (2018) 143: 1021-1027 [PMID:29232579] |
| ChEMBL | Inhibition of NAE in human HCT-116 cells incubated for 1 hr by Western blot analysis | B | 7.52 | pEC50 | 30 | nM | EC50 | J Med Chem (2021) 64: 6161-6178 [PMID:33857374] |
| NEDD8-activating enzyme E1 catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2016430] [UniProtKB: Q8TBC4] | ||||||||
| ChEMBL | Inhibition of human recombinant His-tagged NAE1 expressed in baculovirus expression system after 90 mins in presence of FLAG-tagged NEDD8 by TR-FRET assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2018) 61: 2680-2693 [PMID:29547696] |
| NEDD8-activating enzyme E1 regulatory subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2016431] [UniProtKB: Q13564] | ||||||||
| ChEMBL | Inhibition of NAE (unknown origin)-mediated neddylation assessed as suppression of cullin1-Nedd8 adduct formation preincubated for 10 mins followed by ATP addition and measured after 30 mins by immunoblot analysis | B | 6.74 | pIC50 | 180 | nM | IC50 | Eur J Med Chem (2021) 210: 112964-112964 [PMID:33129593] |
| SUMO-activating enzyme in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095174] [UniProtKB: Q9UBE0, Q9UBT2] | ||||||||
| ChEMBL | Inhibition of SAE1/UBA2 in human HCT-116 cells assessed as reduction in Ubc9-SUMO level incubated for 24 hrs by immunoblot analysis | B | 5.09 | pIC50 | 8200 | nM | IC50 | Eur J Med Chem (2022) 231: 114156-114156 [PMID:35131538] |
| ChEMBL | Inhibition of SAE (unknown origin) assessed as decrease in formation of E2-UBL thioester reaction product | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2018) 61: 3239-3252 [PMID:28505447] |
| Ubiquitin-like modifier-activating enzyme 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5169143] [UniProtKB: Q02053] | ||||||||
| ChEMBL | Inhibition of mouse UAE1 in human HCT-116 cells assessed as reduction in Ubc10-Ub thioester level incubated for 24 hrs by immunoblot analysis | B | 5.82 | pIC50 | 1500 | nM | IC50 | Eur J Med Chem (2022) 231: 114156-114156 [PMID:35131538] |
| Ubiquitin-like modifier-activating enzyme 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321622] [UniProtKB: A0AVT1] | ||||||||
| ChEMBL | Inhibition of His-tagged UBA6 (unknown origin) expressed in sf9 insect cells | B | 5.74 | pIC50 | 1800 | nM | IC50 | Eur J Med Chem (2022) 231: 114156-114156 [PMID:35131538] |
| ChEMBL | Inhibition of UBA6 (unknown origin) assessed as decrease in formation of E2-UBL thioester reaction product | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2018) 61: 3239-3252 [PMID:28505447] |
| Ubiquitin-like modifier-activating enzyme ATG7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321621] [UniProtKB: O95352] | ||||||||
| ChEMBL | Inhibition of His-tagged ATG7 (unknown origin) expressed in sf9 insect cells | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2022) 231: 114156-114156 [PMID:35131538] |
| ChEMBL | Inhibition of ATG7 (unknown origin) assessed as decrease in formation of E2-UBL thioester reaction product | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2018) 61: 3239-3252 [PMID:28505447] |
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]
