Cloned (Comment) | Organism |
---|---|
expression in Cos-1 cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one | competitive | Homo sapiens | |
celecoxib | synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.050 mM in fluorometric assay, in vitro IC50: 0.050 mM in fluorometric assay | Homo sapiens | |
Flufenamic acid | synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0040 mM in fluorometric assay, in vitro IC50: 0.00031 mM in fluorometric assay | Homo sapiens | |
Ibuprofen | synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.017 mM in fluorometric assay, in vitro IC50: 0.009 mM in fluorometric assay | Homo sapiens | |
naproxen | synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0094 mM in fluorometric assay, 0.016 mM in radiometric assay, in vitro IC50: 0.0027 mM in fluorometric assay | Homo sapiens | |
ursodeoxycholate | natural inhibitor, in vivo IC50: 0.00024 mM in fluorometric assay, 0.00014 mM in radiometric assay, in vitro IC50: 0.000049 mM in fluorometric assay | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0013 | - |
5alpha-dihydrotestosterone | recombinant enzyme in intact COS-1 cells | Homo sapiens | |
0.003 | - |
9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one | recombinant enzyme in intact COS-1 cells | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
5alpha-dihydrotestosterone + NADPH + H+ | Homo sapiens | inactivation of the potent androgen in human prostate, fluorometric activity measurement in intact cells, overview | 5alpha-androstan-3alpha,17beta-diol + NADP+ | - |
? | |
9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADPH | Homo sapiens | competitive substrate, fluorometric activity measurement in intact cells, overview | 9-[hydroxy(phenyl)methyl]-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADP+ | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
prostate gland | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
5alpha-dihydrotestosterone + NADPH + H+ | inactivation of the potent androgen in human prostate, fluorometric activity measurement in intact cells, overview | Homo sapiens | 5alpha-androstan-3alpha,17beta-diol + NADP+ | - |
? | |
5alpha-dihydrotestosterone + NADPH + H+ | i.e. DHT | Homo sapiens | 5alpha-androstan-3alpha,17beta-diol + NADP+ | - |
? | |
9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADPH | competitive substrate, fluorometric activity measurement in intact cells, overview | Homo sapiens | 9-[hydroxy(phenyl)methyl]-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADP+ | - |
? | |
9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADPH | competitive substrate | Homo sapiens | 9-[hydroxy(phenyl)methyl]-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADP+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
AKR1C2 | - |
Homo sapiens |
More | cf. EC 1.1.1.50, the enzyme belongs to the aldo-keto reductase, AKR, superfamily | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000049 | - |
natural inhibitor, in vivo IC50: 0.00024 mM in fluorometric assay, 0.00014 mM in radiometric assay, in vitro IC50: 0.000049 mM in fluorometric assay | Homo sapiens | ursodeoxycholate | |
0.00031 | - |
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0040 mM in fluorometric assay, in vitro IC50: 0.00031 mM in fluorometric assay | Homo sapiens | Flufenamic acid | |
0.0027 | - |
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0094 mM in fluorometric assay, 0.016 mM in radiometric assay, in vitro IC50: 0.0027 mM in fluorometric assay | Homo sapiens | naproxen | |
0.009 | - |
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.017 mM in fluorometric assay, in vitro IC50: 0.009 mM in fluorometric assay | Homo sapiens | Ibuprofen | |
0.05 | - |
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.050 mM in fluorometric assay, in vitro IC50: 0.050 mM in fluorometric assay | Homo sapiens | celecoxib |