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| ChEMBL ligand: CHEMBL5199076 (Lunresertib, Rp 6306, Rp-6306, RP-6306, RP6306) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CREB binding lysine acetyltransferase/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793] | ||||||||
| ChEMBL | Inhibition of CREBBP (unknown origin) by TR-FRET assay | B | 6.52 | pIC50 | 300 | nM | IC50 | ACS Med Chem Lett (2024) 15: 436-440 [PMID:38628791] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Inhibition of CDK1 phosphorylation at Thr14 residue in human HCC1569 cells incubated for 6 hrs by Western blot analysis | B | 7.28 | pIC50 | 52 | nM | IC50 | J Med Chem (2024) 67: 420-432 [PMID:38146659] |
| protein kinase, membrane associated tyrosine/threonine 1/Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640] | ||||||||
| ChEMBL | Inhibition of N-terminal recombinant PKMYT1 (76 to 362 residues) in CCNE1 amplified human FU-OV-1 cells assessed as phosphorylation of CDK1 at Thr14 incubated for 2 hrs by AlphaLisa assay | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2022) 65: 10251-10284 [PMID:35880755] |
| ChEMBL | Inhibition of recombinant human GST-tagged PKMYT1 (75 to 362 residues) expressed in insect cells using GTDEGIYDVPLLG as substrate preincubated for 15 mins followed by substrate and ATP addition and measured after 1 hr by ADP-Glo kinase assay | B | 8.08 | pIC50 | 8.4 | nM | IC50 | J Med Chem (2024) 67: 15816-15836 [PMID:39163619] |
| ChEMBL | Inhibition of full length Nano-luc fused PKMYT1 in human HEK-293T cells incubated for 2 hrs by cell based NanoBRET target engagement assay | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2022) 65: 10251-10284 [PMID:35880755] |
| Myelin transcription factor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331044] [UniProtKB: Q01538] | ||||||||
| ChEMBL | Inhibition of human recombinant MYT1 incubated for 60 mins in presence of tracer178 by HTRF analysis | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2024) 67: 420-432 [PMID:38146659] |
| WEE1 G2 checkpoint kinase/Wee1-like protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5491] [GtoPdb: 2278] [UniProtKB: P30291] | ||||||||
| ChEMBL | Inhibition of human recombinant Wee1 preincubated with compound for for 15 mins followed by ATP addition and measured after 60 mins by ADP Glo luminescent assay | B | 6.98 | pIC50 | 104 | nM | IC50 | J Med Chem (2024) 67: 420-432 [PMID:38146659] |
ChEMBL data shown on this page come from version 36:
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]