BDBM195609 CPI-4203
SMILES: CCc1c([nH]c2c(cnn2c1=O)C#N)-c1ccccc1C
InChI Key: InChIKey=OXELDRCVUWWSFZ-UHFFFAOYSA-N
Data: 11 IC50
Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kcal/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM195609 (CPI-4203) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | 248 | n/a | n/a | n/a | n/a | 7.0 | n/a |
Genentech Inc | Assay Description Time-resolved fluorescence resonance energy transfer (TR-FRET) assays were carried out using full-length KDM5 enzymes in 384-well black ProxiPlates (... | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM195609 (CPI-4203) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | 1.50E+3 | n/a | n/a | n/a | n/a | 7.0 | n/a |
Genentech Inc | Assay Description Time-resolved fluorescence resonance energy transfer (TR-FRET) assays were carried out using full-length KDM5 enzymes in 384-well black ProxiPlates (... | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5B (Homo sapiens (Human)) | BDBM195609 (CPI-4203) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | 77 | n/a | n/a | n/a | n/a | 7.0 | n/a |
Genentech Inc | Assay Description Time-resolved fluorescence resonance energy transfer (TR-FRET) assays were carried out using full-length KDM5 enzymes in 384-well black ProxiPlates (... | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5C (Homo sapiens (Human)) | BDBM195609 (CPI-4203) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | 397 | n/a | n/a | n/a | n/a | 7.0 | n/a |
Genentech Inc | Assay Description Time-resolved fluorescence resonance energy transfer (TR-FRET) assays were carried out using full-length KDM5 enzymes in 384-well black ProxiPlates (... | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 2B (Homo sapiens (Human)) | BDBM195609 (CPI-4203) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | >2.50E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Inc | Assay Description TR-FRET assays similar to those described above for KDM5 enzymes were carried out with full-length KDM2B, KDM3B, KDM4C, KDM6A and KDM7B. | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM195609 (CPI-4203) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | 206 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM5A (unknown origin) using ART(Kme3)QTARKSTGGKAPRKQLA-NovaTagPEG-biotin/1 uM 2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 4C (KDM4C) (Homo sapiens (Human)) | BDBM195609 (CPI-4203) | PDB GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | 3.00E+3 | n/a | n/a | n/a | n/a | 7.5 | n/a |
Genentech Inc | Assay Description High-throughput MS assays were carried out using truncated KDM4C in 384-well V-bottom polypropylene plates (Greiner, Inc.). His-tagged recombinant KD... | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 6A (KDM6A) (Homo sapiens (Human)) | BDBM195609 (CPI-4203) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | >2.50E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Inc | Assay Description TR-FRET assays similar to those described above for KDM5 enzymes were carried out with full-length KDM2B, KDM3B, KDM4C, KDM6A and KDM7B. | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone lysine demethylase PHF8 (Homo sapiens (Human)) | BDBM195609 (CPI-4203) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | >2.50E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Inc | Assay Description TR-FRET assays similar to those described above for KDM5 enzymes were carried out with full-length KDM2B, KDM3B, KDM4C, KDM6A and KDM7B. | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM195609 (CPI-4203) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | 206 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM5A (unknown origin) using ART(Kme3)QTARKSTGGKAPRKQLA-NovaTagPEG-biotin/1 uM 2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 3B (KDM3B) (Homo sapiens (Human)) | BDBM195609 (CPI-4203) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | >2.50E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Inc | Assay Description TR-FRET assays similar to those described above for KDM5 enzymes were carried out with full-length KDM2B, KDM3B, KDM4C, KDM6A and KDM7B. | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair |