General Information of the Protein
Protein ID
PT02399
Protein Name
6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3
Secondarily
Protein Name
6PF-2-K/Fru-2,6-P2ase brain/placenta-type isozyme
Renal carcinoma antigen NY-REN-56
iPFK-2
Gene Name
PFKFB3
Sequence
MPLELTQSRVQKIWVPVDHRPSLPRSCGPKLTNSPTVIVMVGLPARGKTYISKKLTRYLNWIGVPTKVFNVGEYRREAVKQYSSYNFFRPDNEEAMKVRKQCALAALRDVKSYLAKEGGQIAVFDATNTTRERRHMILHFAKENDFKAFFIESVCDDPTVVASNIMEVKISSPDYKDCNSAEAMDDFMKRISCYEASYQPLDPDKCDRDLSLIKVIDVGRRFLVNRVQDHIQSRIVYYLMNIHVQPRTIYLCRHGENEHNLQGRIGGDSGLSSRGKKFASALSKFVEEQNLKDLRVWTSQLKSTIQTAEALRLPYEQWKALNEIDAGVCEELTYEEIRDTYPEEYALREQDKYYYRYPTGESYQDLVQRLEPVIMELERQENVLVICHQAVLRCLLAYFLDKSAEEMPYLKCPLHTVLKLTPVAYGCRVESIYLNVESVCTHRERSEDAKKGPNPLMRRNSVTPLASPEPTKKPRINSFEEHVASTSAALPSCLPPEVPTQLPGQNMKGSRSSADSSRKH
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Enzyme
Function
Catalyzes both the synthesis and degradation of fructose 2,6-bisphosphate.
    Show/Hide
Uniprot ID
Primary ID:
Q16875

Secondarily ID:
B7Z955
O43622
O75902
Q5VX15
Q5VX18
Q5VX19
    Show/Hide
Ensembl ID
ENSG00000170525
HGNC ID
HGNC:8874
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000068 , A-549
Compound ID Compound Name Compound Formula
CP0084905
(2S)-N-[4-[3-cyano-1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]indazol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C25H24N6O3
 1
1
IC50 = 67 nM
   TI
   LI
   LO
   TS
CP0072063
(2S)-N-[4-[3-cyano-1-(2-methyl-1-oxo-3H-isoindol-5-yl)indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C29H25N5O3
 2
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
2
IC50 = 2180 nM
   TI
   LI
   LO
   TS
CP0084903
(2S)-N-[4-[3-cyano-1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C26H25N5O3
 2
1
IC50 = 281 nM
   TI
   LI
   LO
   TS
2
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0084899
(2S)-N-[4-[3-cyano-1-(2-methylpropyl)indazol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C23H25N5O2
 2
1
IC50 = 297 nM
   TI
   LI
   LO
   TS
2
IC50 = 15400 nM
   TI
   LI
   LO
   TS
CP0084901
(2S)-N-[4-[3-cyano-1-(2-methylpropyl)indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C24H26N4O2
 2
1
IC50 = 343 nM
   TI
   LI
   LO
   TS
2
IC50 = 5770 nM
   TI
   LI
   LO
   TS
CP0259656
(2S)-N-[4-[3-cyano-1-(oxan-4-ylmethyl)indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C26H28N4O3
 2
1
IC50 = 633 nM
   TI
   LI
   LO
   TS
2
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0072065
(2S)-N-[4-[1-methyl-3-(1-methylpyrazol-4-yl)indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C24H25N5O2
 2
1
IC50 = 979 nM
   TI
   LI
   LO
   TS
2
IC50 = 9710 nM
   TI
   LI
   LO
   TS
CP0246772
(2S)-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C22H22N4O2
 2
1
IC50 = 3050 nM
   TI
   LI
   LO
   TS
2
IC50 = 12000 nM
   TI
   LI
   LO
   TS
CP0119441
(2S)-N-[4-(1-benzyl-3-cyanoindol-5-yl)oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C27H24N4O2
 1
1
IC50 = 6950 nM
   TI
   LI
   LO
   TS
CP0524302
(2S)-N-[4-[3-cyano-1-[2-(dimethylamino)ethyl]indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C24H27N5O2
 2
1
IC50 = 7480 nM
   TI
   LI
   LO
   TS
2
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0282315
(2S)-N-[4-(3-cyano-1-phenylindol-5-yl)oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C26H22N4O2
 1
1
IC50 = 8710 nM
   TI
   LI
   LO
   TS
CP0111468
2-amino-N-[4-(2-amino-1-benzyl-3-cyanoindol-5-yl)oxyphenyl]acetamide
   Show/Hide
C24H21N5O2
 2
1
IC50 = 12600 nM
   TI
   LI
   LO
   TS
2
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0072066
(2S)-N-[4-[[3-cyano-1-(2-methylpropyl)indol-5-yl]-methylamino]phenyl]pyrrolidine-2-carboxamide
   Show/Hide
C25H29N5O
 2
1
IC50 = 13700 nM
   TI
   LI
   LO
   TS
2
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0172548
(2S)-N-[4-[3-cyano-1-(2-methylpropyl)indol-5-yl]sulfanylphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C24H26N4OS
 1
1
IC50 = 14000 nM
   TI
   LI
   LO
   TS
CP0051690
(2S)-N-[4-[3-cyano-1-[2-(methylamino)-2-oxoethyl]indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C23H23N5O3
 2
1
IC50 = 14000 nM
   TI
   LI
   LO
   TS
2
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0172543
2-amino-N-[4-[2-amino-3-cyano-1-(2-methylpropyl)indol-5-yl]oxyphenyl]acetamide
   Show/Hide
C21H23N5O2
 2
1
IC50 = 16400 nM
   TI
   LI
   LO
   TS
2
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0084898
(2S)-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]azetidine-2-carboxamide
   Show/Hide
C21H20N4O2
 1
1
IC50 = 19600 nM
   TI
   LI
   LO
   TS
CP0282316
(2S)-N-[4-[3-cyano-1-(2-methylpropyl)indol-5-yl]sulfonylphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C24H26N4O3S
 2
1
IC50 = 24700 nM
   TI
   LI
   LO
   TS
2
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0051689
(2S)-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]-N-methylpyrrolidine-2-carboxamide
   Show/Hide
C23H24N4O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0051691
(2S)-N-[4-[[3-cyano-1-(2-methylpropyl)indol-5-yl]amino]phenyl]pyrrolidine-2-carboxamide
   Show/Hide
C24H27N5O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0072062
N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]-2-(methylamino)acetamide
   Show/Hide
C20H20N4O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0072899
2-amino-N-[4-(2-amino-3-cyano-1-methylindol-5-yl)oxyphenyl]acetamide
   Show/Hide
C18H17N5O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0117230
2-amino-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]acetamide
   Show/Hide
C19H18N4O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0154584
2-amino-N-[4-[2-amino-3-cyano-1-[2-(dimethylamino)-2-oxoethyl]indol-5-yl]oxyphenyl]acetamide
   Show/Hide
C21H22N6O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0170151
N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]-2-(dimethylamino)acetamide
   Show/Hide
C21H22N4O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0171547
2-amino-N-[4-[[3-(1-methylpyrazol-4-yl)-1H-indazol-5-yl]oxy]phenyl]acetamide
   Show/Hide
C19H18N6O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0172545
(2R)-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C22H22N4O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0317360
(2S)-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]-N-methyl-5-oxopyrrolidine-2-carboxamide
   Show/Hide
C23H22N4O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0488237
(2S)-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]piperidine-2-carboxamide
   Show/Hide
C23H24N4O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0780865
(2S)-N-[4-[[3-(1-Methylpyrazol-4-yl)-1H-indol-5-yl]oxy]-phenyl]pyrrolidine-2-carboxamide
   Show/Hide
C23H23N5O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0051697
(2S)-N-[4-[[3-cyano-1-(2-methylpropyl)indol-5-yl]methyl]phenyl]pyrrolidine-2-carboxamide
   Show/Hide
C25H28N4O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0157996
2-amino-N-[4-(2-amino-3-cyano-1-ethylindol-5-yl)oxyphenyl]acetamide
   Show/Hide
C19H19N5O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0709800
(2S)-2-Amino-N-[4-[(2-amino-3-cyano-1H-indol-5-yl)oxy]phenyl]-3-hydroxy-propanamide
   Show/Hide
C18H17N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0084905
(2S)-N-[4-[3-cyano-1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]indazol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C25H24N6O3
 1
1 IC50 = 3 nM
CP0084899
(2S)-N-[4-[3-cyano-1-(2-methylpropyl)indazol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C23H25N5O2
 1
1 IC50 = 4 nM
CP0072063
(2S)-N-[4-[3-cyano-1-(2-methyl-1-oxo-3H-isoindol-5-yl)indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C29H25N5O3
 1
1 IC50 = 8 nM
CP0084903
(2S)-N-[4-[3-cyano-1-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C26H25N5O3
 1
1 IC50 = 11 nM
CP0119441
(2S)-N-[4-(1-benzyl-3-cyanoindol-5-yl)oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C27H24N4O2
 1
1 IC50 = 20 nM
CP0072065
(2S)-N-[4-[1-methyl-3-(1-methylpyrazol-4-yl)indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C24H25N5O2
 1
1 IC50 = 21 nM
CP0084901
(2S)-N-[4-[3-cyano-1-(2-methylpropyl)indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C24H26N4O2
 1
1 IC50 = 23 nM
CP0282315
(2S)-N-[4-(3-cyano-1-phenylindol-5-yl)oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C26H22N4O2
 1
1 IC50 = 27 nM
CP0259656
(2S)-N-[4-[3-cyano-1-(oxan-4-ylmethyl)indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C26H28N4O3
 1
1 IC50 = 48 nM
CP0072066
(2S)-N-[4-[[3-cyano-1-(2-methylpropyl)indol-5-yl]-methylamino]phenyl]pyrrolidine-2-carboxamide
   Show/Hide
C25H29N5O
 1
1 IC50 = 75 nM
CP0084898
(2S)-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]azetidine-2-carboxamide
   Show/Hide
C21H20N4O2
 1
1 IC50 = 86 nM
CP0111468
2-amino-N-[4-(2-amino-1-benzyl-3-cyanoindol-5-yl)oxyphenyl]acetamide
   Show/Hide
C24H21N5O2
 1
1 IC50 = 104 nM
CP0051690
(2S)-N-[4-[3-cyano-1-[2-(methylamino)-2-oxoethyl]indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C23H23N5O3
 1
1 IC50 = 111 nM
CP0172548
(2S)-N-[4-[3-cyano-1-(2-methylpropyl)indol-5-yl]sulfanylphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C24H26N4OS
 1
1 IC50 = 111 nM
CP0246772
(2S)-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C22H22N4O2
 1
1 IC50 = 112 nM
CP0780865
(2S)-N-[4-[[3-(1-Methylpyrazol-4-yl)-1H-indol-5-yl]oxy]-phenyl]pyrrolidine-2-carboxamide
   Show/Hide
C23H23N5O2
 1
1 IC50 = 114 nM
CP0172543
2-amino-N-[4-[2-amino-3-cyano-1-(2-methylpropyl)indol-5-yl]oxyphenyl]acetamide
   Show/Hide
C21H23N5O2
 1
1 IC50 = 177 nM
CP0051697
(2S)-N-[4-[[3-cyano-1-(2-methylpropyl)indol-5-yl]methyl]phenyl]pyrrolidine-2-carboxamide
   Show/Hide
C25H28N4O
 1
1 IC50 = 199 nM
CP0524302
(2S)-N-[4-[3-cyano-1-[2-(dimethylamino)ethyl]indol-5-yl]oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C24H27N5O2
 1
1 IC50 = 256 nM
CP0154584
2-amino-N-[4-[2-amino-3-cyano-1-[2-(dimethylamino)-2-oxoethyl]indol-5-yl]oxyphenyl]acetamide
   Show/Hide
C21H22N6O3
 1
1 IC50 = 343 nM
CP0171547
2-amino-N-[4-[[3-(1-methylpyrazol-4-yl)-1H-indazol-5-yl]oxy]phenyl]acetamide
   Show/Hide
C19H18N6O2
 1
1 IC50 = 496 nM
CP0157996
2-amino-N-[4-(2-amino-3-cyano-1-ethylindol-5-yl)oxyphenyl]acetamide
   Show/Hide
C19H19N5O2
 1
1 IC50 = 514 nM
CP0317360
(2S)-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]-N-methyl-5-oxopyrrolidine-2-carboxamide
   Show/Hide
C23H22N4O3
 1
1 IC50 = 531 nM
CP0117230
2-amino-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]acetamide
   Show/Hide
C19H18N4O2
 1
1 IC50 = 562 nM
CP0709800
(2S)-2-Amino-N-[4-[(2-amino-3-cyano-1H-indol-5-yl)oxy]phenyl]-3-hydroxy-propanamide
   Show/Hide
C18H17N5O3
 1
1 IC50 = 575 nM
CP0072899
2-amino-N-[4-(2-amino-3-cyano-1-methylindol-5-yl)oxyphenyl]acetamide
   Show/Hide
C18H17N5O2
 1
1 IC50 = 815 nM
CP0072062
N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]-2-(methylamino)acetamide
   Show/Hide
C20H20N4O2
 1
1 IC50 = 830 nM
CP0051691
(2S)-N-[4-[[3-cyano-1-(2-methylpropyl)indol-5-yl]amino]phenyl]pyrrolidine-2-carboxamide
   Show/Hide
C24H27N5O
 1
1 IC50 = 1570 nM
CP0488237
(2S)-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]piperidine-2-carboxamide
   Show/Hide
C23H24N4O2
 1
1 IC50 = 2200 nM
CP0170151
N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]-2-(dimethylamino)acetamide
   Show/Hide
C21H22N4O2
 1
1 IC50 = 9830 nM
CP0051689
(2S)-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]-N-methylpyrrolidine-2-carboxamide
   Show/Hide
C23H24N4O2
 1
1 IC50 = 23100 nM
CP0282316
(2S)-N-[4-[3-cyano-1-(2-methylpropyl)indol-5-yl]sulfonylphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C24H26N4O3S
 1
1 IC50 = 37700 nM
CP0172545
(2R)-N-[4-(3-cyano-1-ethylindol-5-yl)oxyphenyl]pyrrolidine-2-carboxamide
   Show/Hide
C22H22N4O2
 1
1 IC50 = 70900 nM
Clinical Information about the Protein
Target 1 ( Renal carcinoma antigen NY-REN-56 (PFKFB3) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Pulmonary fibrosis [ICD-11: CB03.4]
Investigative Drug(s) 1 Investigative Drug  1
1 3PO Investigative
Pulmonary fibrosis