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Target
PC4 and SFRS1-interacting protein
Ligand
BDBM61724
Substrate
n/a
Meas. Tech.
Counterscreen for inhibitors of LEDGF/p75-dependent integration: TR-FRET-based biochemical high throughput dose response counterscreen assay to identify activators of HIV-1 Integrase multimerization
IC50
663.1±n/a nM
Citation
 PubChem, PC Counterscreen for inhibitors of LEDGF/p75-dependent integration: TR-FRET-based biochemical high throughput dose response counterscreen assay to identify activators of HIV-1 Integrase multimerization PubChem Bioassay (2014)[AID] 
Target
Name:
PC4 and SFRS1-interacting protein
Synonyms:
DFS70 | LEDGF | LEDGF/p75 | PSIP1 | PSIP1_HUMAN | PSIP2 | lens epithelium-derived growth factor p75
Type:
Enzyme Catalytic Domain
Mol. Mass.:
60120.68
Organism:
Homo sapiens (Human)
Description:
gi_6708281
Residue:
530
Sequence:
MTRDFKPGDLIFAKMKGYPHWPARVDEVPDGAVKPPTNKLPIFFFGTHETAFLGPKDIFPYSENKEKYGKPNKRKGFNEGLWEIDNNPKVKFSSQQAATKQSNASSDVEVEEKETSVSKEDTDHEEKASNEDVTKAVDITTPKAARRGRKRKAEKQVETEEAGVVTTATASVNLKVSPKRGRPAATEVKIPKPRGRPKMVKQPCPSESDIITEEDKSKKKGQEEKQPKKQPKKDEEGQKEEDKPRKEPDKKEGKKEVESKRKNLAKTGVTSTSDSEEEGDDQEGEKKRKGGRNFQTAHRRNMLKGQHEKEAADRKRKQEEQMETEQQNKDEGKKPEVKKVEKKRETSMDSRLQRIHAEIKNSLKIDNLDVNRCIEALDELASLQVTMQQAQKHTEMITTLKKIRRFKVSQVIMEKSTMLYNKFKNMFLVGEGDSVITQVLNKSLAEQRQHEEANKTKDQGKKGPNKKLEKEQTGSKTLNGGSDAQDGNQPQHNGESNEDSKDNHEASTKKKPSSEERETEISLKDSTLDN
  
Inhibitor
Name:
BDBM61724
Synonyms:
(8S)-3-(3-methacrylamidophenyl)-7-(1-methylcyclopropanecarbonyl)-1-oxa-2,7-diazaspiro[4.4]non-2-ene-8-carboxamide | (8S)-7-(1-methylcyclopropanecarbonyl)-3-[3-(2-methylprop-2-enoylamino)phenyl]-1-oxa-2,7-diazaspiro[4.4]non-2-ene-8-carboxamide | (8S)-7-(1-methylcyclopropyl)carbonyl-3-[3-(2-methylprop-2-enoylamino)phenyl]-1-oxa-2,7-diazaspiro[4.4]non-2-ene-8-carboxamide | (8S)-7-[(1-methylcyclopropyl)-oxomethyl]-3-[3-[(2-methyl-1-oxoprop-2-enyl)amino]phenyl]-1-oxa-2,7-diazaspiro[4.4]non-2-ene-8-carboxamide | MLS000562014 | SMR000390649 | cid_16745487
Type:
Small organic molecule
Emp. Form.:
C22H26N4O4
Mol. Mass.:
410.4662
SMILES:
CC(=C)C(=O)Nc1cccc(c1)C1=NOC2(C[C@H](N(C2)C(=O)C2(C)CC2)C(N)=O)C1 |t:13|
Structure:
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