lunresertib [Ligand Id: 13211] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL5199076 (Lunresertib, Rp 6306, Rp-6306, RP-6306)
  • CREB binding protein/CREB-binding protein in Human [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
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  • protein kinase, membrane associated tyrosine/threonine 1/Tyrosine- and threonine-specific cdc2-inhibitory kinase in Human [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CREB binding protein/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]
protein kinase, membrane associated tyrosine/threonine 1/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 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]

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]