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Target
6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3
Ligand
BDBM50209568
Substrate
n/a
Meas. Tech.
ChEMBL_1286130 (CHEMBL3106987)
IC50
670±n/a nM
Citation
 Brooke, DG; van Dam, EM; Watts, CK; Khoury, A; Dziadek, MA; Brooks, H; Graham, LJ; Flanagan, JU; Denny, WA Targeting the Warburg Effect in cancer; relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3). Bioorg Med Chem 22:1029-39 (2014) [PubMed]  Article 
Target
Name:
6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3
Synonyms:
6-phosphofructo-2-kinase | 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 | 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) | 6PF-2-K/Fru-2,6-P2ase 3 | 6PF-2-K/Fru-2,6-P2ase brain/placenta-type isozyme | F263_HUMAN | Fructose-2,6-bisphosphatase | PFK/FBPase 3 | PFKFB3 | Renal carcinoma antigen NY-REN-56 | iPFK-2
Type:
Enzyme
Mol. Mass.:
59620.59
Organism:
Homo sapiens (Human)
Description:
Q16875
Residue:
520
Sequence:
MPLELTQSRVQKIWVPVDHRPSLPRSCGPKLTNSPTVIVMVGLPARGKTYISKKLTRYLNWIGVPTKVFNVGEYRREAVKQYSSYNFFRPDNEEAMKVRKQCALAALRDVKSYLAKEGGQIAVFDATNTTRERRHMILHFAKENDFKAFFIESVCDDPTVVASNIMEVKISSPDYKDCNSAEAMDDFMKRISCYEASYQPLDPDKCDRDLSLIKVIDVGRRFLVNRVQDHIQSRIVYYLMNIHVQPRTIYLCRHGENEHNLQGRIGGDSGLSSRGKKFASALSKFVEEQNLKDLRVWTSQLKSTIQTAEALRLPYEQWKALNEIDAGVCEELTYEEIRDTYPEEYALREQDKYYYRYPTGESYQDLVQRLEPVIMELERQENVLVICHQAVLRCLLAYFLDKSAEEMPYLKCPLHTVLKLTPVAYGCRVESIYLNVESVCTHRERSEDAKKGPNPLMRRNSVTPLASPEPTKKPRINSFEEHVASTSAALPSCLPPEVPTQLPGQNMKGSRSSADSSRKH
  
Inhibitor
Name:
BDBM50209568
Synonyms:
4',7,8-trihydroxyisoflavone | 7,8,4'-trihydroxyisoflavone | 7,8-dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one | CHEMBL242739 | IR-301
Type:
Small organic molecule
Emp. Form.:
C15H10O5
Mol. Mass.:
270.2369
SMILES:
Oc1ccc(cc1)-c1coc2c(O)c(O)ccc2c1=O
Structure:
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