Protein Variants | Comment | Organism |
---|---|---|
F239A | the IC50 of CA28a against the F239A mutant enzyme is about 500% larger than against wild type protein | Homo sapiens |
N59A | CA28a exhibits the same IC50 against the N59A mutant enzyme ass against wild type protein | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(4bR,8aS)-4b-(5-acetyl-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-5,6,7,8,8a,9-hexahydrophenanthrene-3,4,10(4bH)-trione | - |
Homo sapiens | |
(4bR,8aS)-4b-(5-amino-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol | - |
Homo sapiens | |
(4bR,8aS)-4b-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol | - |
Homo sapiens | |
(4bR,8aS)-4b-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-5,6,7,8,8a,9-hexahydrophenanthrene-3,4,10(4bH)-trione | - |
Homo sapiens | |
(4bR,8aS)-4b-(5-[(1S)-1-[(hydroxymethyl)amino]ethyl]-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol | - |
Homo sapiens | |
(4bR,8aS)-4b-[5-(4-bromophenyl)-1,3,4-oxadiazol-2-yl]-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol | - |
Homo sapiens | |
(4bR,8aS)-4b-[5-(4-bromophenyl)-1,3,4-oxadiazol-2-yl]-8,8-dimethyl-2-(propan-2-yl)-5,6,7,8,8a,9-hexahydrophenanthrene-3,4,10(4bH)-trione | - |
Homo sapiens | |
(4bR,8aS)-4b-[5-[(dimethylamino)methyl]-1,3,4-oxadiazol-2-yl]-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol | - |
Homo sapiens | |
11,12-dihydroxy-7,20-epoxyabieta-8,11,13-trien-20-one | - |
Homo sapiens | |
11,12-dihydroxy-N-(2-hydroxyethyl)abieta-8(14),9(11),12-trien-20-amide | - |
Homo sapiens | |
11,12-dihydroxy-N-methylabieta-8(14),9(11),12-trien-20-amide | - |
Homo sapiens | |
11,12-dihydroxy-N-[(pyridin-3-yl)methyl]abieta-8(14),9(11),12-trien-20-amide | - |
Homo sapiens | |
11,12-dihydroxy-N-[3-(1H-imidazol-1-yl)propyl]abieta-8(14),9(11),12-trien-20-amide | - |
Homo sapiens | |
11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide | - |
Homo sapiens | |
12-hydroxy-11,20-epoxyabieta-8(14),9(11),12-trien-20-one | - |
Homo sapiens | |
2-[11,12-dihydroxy-20-oxoabieta-8(14),9(11),12-trien-20-yl]hydrazine-1-carboxamide | - |
Homo sapiens | |
4-[5-[(4aR,10aS)-5,6-dihydroxy-1,1-dimethyl-7-(propan-2-yl)-1,3,4,9,10,10a-hexahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]benzonitrile | - |
Homo sapiens | |
6,20-epoxyabieta-8,13-diene-7,11,12,20-tetrone | - |
Homo sapiens | |
7,20-epoxyabieta-8(14),9(11),12-triene-11,12-diol | - |
Homo sapiens | |
7,20-epoxyabieta-8,13-diene-11,12,20-trione | - |
Homo sapiens | |
7,20-epoxyabieta-8,13-diene-11,12-dione | - |
Homo sapiens | |
abieta-8(14),9(11),12-triene-11,12,20-triol | - |
Homo sapiens | |
methyl 11,12-dihydroxy-7-(phenylsulfanyl)abieta-8(14),9(11),12-trien-20-oate | - |
Homo sapiens | |
methyl 11,12-dihydroxy-7-methoxyabieta-8(14),9(11),12-trien-20-oate | - |
Homo sapiens | |
methyl 11,12-dihydroxy-7-oxoabieta-8(14),9(11),12-trien-20-oate | - |
Homo sapiens | |
methyl 11,12-dihydroxy-7-[(2-hydroxyethyl)sulfanyl]abieta-8(14),9(11),12-trien-20-oate | - |
Homo sapiens | |
methyl 11,12-dihydroxyabieta-7,9(11),13-trien-20-oate | - |
Homo sapiens | |
methyl 11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate | - |
Homo sapiens | |
methyl 11-[[tert-butyl(dimethyl)silyl]oxy]-12-hydroxyabieta-8(14),9(11),12-trien-20-oate | - |
Homo sapiens | |
methyl 7,11,12-trioxoabieta-8,13-dien-20-oate | - |
Homo sapiens | |
methyl 7-(butylsulfanyl)-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate | - |
Homo sapiens | |
methyl 7-ethoxy-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate | - |
Homo sapiens | |
methyl 7-ethoxy-11,12-dioxoabieta-8,13-dien-20-oate | - |
Homo sapiens | |
methyl 7-tert-butoxy-11,12-dioxoabieta-8,13-dien-20-oate | - |
Homo sapiens | |
methyl 7-[(2-hydroxyethyl)sulfanyl]-11,12-dioxoabieta-8,13-dien-20-oate | - |
Homo sapiens | |
N'-(4-bromobenzoyl)-11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide | - |
Homo sapiens | |
N'-acetyl-11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide | - |
Homo sapiens | |
N-acetyl-S-((4aR,10aS)-5,6-dihydroxy-7-isopropyl-4a-(methoxycarbonyl)-1,1-dimethyl-1,2,3,4,4a,9,10,10a-octahydrophenanthren-9-yl)-L-cysteine | - |
Homo sapiens | |
N-benzyl-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-amide | - |
Homo sapiens | |
N-[2-(dimethylamino)ethyl]-11,12-dihydroxy-7-oxoabieta-8(14),9(11),12-trien-20-amide | - |
Homo sapiens | |
N-[2-(dimethylamino)ethyl]-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-amide | - |
Homo sapiens | |
tert-butyl [(1R)-1-amino-2-[2-[11,12-dihydroxy-20-oxoabieta-8(14),9(11),12-trien-20-yl]hydrazinyl]-2-oxoethyl]carbamate | - |
Homo sapiens | |
tert-butyl [(1R)-1-[5-[(4aR,10aS)-5,6-dihydroxy-1,1-dimethyl-9-oxo-7-(propan-2-yl)-1,3,4,9,10,10a-hexahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]ethyl]carbamate | - |
Homo sapiens | |
tert-butyl [(1S)-1-[5-[(4aR,10aS)-1,1-dimethyl-5,6,9-trioxo-7-(propan-2-yl)-1,3,4,5,6,9,10,10a-octahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]ethyl]carbamate | - |
Homo sapiens | |
tert-butyl [(1S)-1-[5-[(4aR,10aS)-5,6-dihydroxy-1,1-dimethyl-7-(propan-2-yl)-1,3,4,9,10,10a-hexahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]ethyl]carbamate | - |
Homo sapiens | |
zoledronate | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
dimethylallyl diphosphate + isopentenyl diphosphate | Homo sapiens | reaction of EC 2.5.1.1, the enzyme catalyzes the condensation of dimethylallyl pyrophosphate and isopentenyl pyrophosphate, forming geranyl pyrophosphate and then farnesyl pyrophosphate | diphosphate + geranyl diphosphate | - |
? | |
geranyl diphosphate + isopentenyl diphosphate | Homo sapiens | reaction of EC 2.5.1.10, the enzyme catalyzes the condensation of dimethylallyl pyrophosphate and isopentenyl pyrophosphate, forming geranyl pyrophosphate and then farnesyl pyrophosphate | diphosphate + (2E,6E)-farnesyl diphosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P14324 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
pancreatic cancer cell line | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
dimethylallyl diphosphate + isopentenyl diphosphate | reaction of EC 2.5.1.1, the enzyme catalyzes the condensation of dimethylallyl pyrophosphate and isopentenyl pyrophosphate, forming geranyl pyrophosphate and then farnesyl pyrophosphate | Homo sapiens | diphosphate + geranyl diphosphate | - |
? | |
dimethylallyl diphosphate + isopentenyl diphosphate | the enzyme catalyzes the condensation of dimethylallyl pyrophosphate and isopentenyl pyrophosphate, forming geranyl pyrophosphate and then farnesyl pyrophosphate | Homo sapiens | diphosphate + geranyl diphosphate | - |
? | |
geranyl diphosphate + isopentenyl diphosphate | reaction of EC 2.5.1.10, the enzyme catalyzes the condensation of dimethylallyl pyrophosphate and isopentenyl pyrophosphate, forming geranyl pyrophosphate and then farnesyl pyrophosphate | Homo sapiens | diphosphate + (2E,6E)-farnesyl diphosphate | - |
? |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
23 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0001 | - |
pH 7.5, 23°C | Homo sapiens | zoledronate | |
0.000194 | - |
pH 7.5, 23°C | Homo sapiens | (4bR,8aS)-4b-(5-[(1S)-1-[(hydroxymethyl)amino]ethyl]-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol | |
0.000234 | - |
pH 7.5, 23°C | Homo sapiens | methyl 7-tert-butoxy-11,12-dioxoabieta-8,13-dien-20-oate | |
0.000252 | - |
pH 7.5, 23°C | Homo sapiens | tert-butyl [(1S)-1-[5-[(4aR,10aS)-1,1-dimethyl-5,6,9-trioxo-7-(propan-2-yl)-1,3,4,5,6,9,10,10a-octahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]ethyl]carbamate | |
0.000289 | - |
pH 7.5, 23°C | Homo sapiens | (4bR,8aS)-4b-(5-acetyl-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-5,6,7,8,8a,9-hexahydrophenanthrene-3,4,10(4bH)-trione | |
0.000335 | - |
pH 7.5, 23°C | Homo sapiens | (4bR,8aS)-4b-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-5,6,7,8,8a,9-hexahydrophenanthrene-3,4,10(4bH)-trione | |
0.000389 | - |
pH 7.5, 23°C | Homo sapiens | 6,20-epoxyabieta-8,13-diene-7,11,12,20-tetrone | |
0.000473 | - |
pH 7.5, 23°C | Homo sapiens | 7,20-epoxyabieta-8,13-diene-11,12,20-trione | |
0.00052 | - |
pH 7.5, 23°C | Homo sapiens | tert-butyl [(1R)-1-amino-2-[2-[11,12-dihydroxy-20-oxoabieta-8(14),9(11),12-trien-20-yl]hydrazinyl]-2-oxoethyl]carbamate | |
0.000523 | - |
pH 7.5, 23°C | Homo sapiens | methyl 7,11,12-trioxoabieta-8,13-dien-20-oate | |
0.000596 | - |
pH 7.5, 23°C | Homo sapiens | 7,20-epoxyabieta-8,13-diene-11,12-dione | |
0.000644 | - |
pH 7.5, 23°C | Homo sapiens | tert-butyl [(1S)-1-[5-[(4aR,10aS)-5,6-dihydroxy-1,1-dimethyl-7-(propan-2-yl)-1,3,4,9,10,10a-hexahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]ethyl]carbamate | |
0.0008 | - |
pH 7.5, 23°C | Homo sapiens | N'-(4-bromobenzoyl)-11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide | |
0.000833 | - |
pH 7.5, 23°C | Homo sapiens | methyl 11,12-dihydroxyabieta-7,9(11),13-trien-20-oate | |
0.000859 | - |
pH 7.5, 23°C | Homo sapiens | (4bR,8aS)-4b-(5-amino-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol | |
0.000865 | - |
pH 7.5, 23°C | Homo sapiens | methyl 11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate | |
0.000914 | - |
pH 7.5, 23°C | Homo sapiens | 11,12-dihydroxy-N-(2-hydroxyethyl)abieta-8(14),9(11),12-trien-20-amide | |
0.0011 | - |
pH 7.5, 23°C | Homo sapiens | (4bR,8aS)-4b-[5-[(dimethylamino)methyl]-1,3,4-oxadiazol-2-yl]-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol | |
0.0011 | - |
pH 7.5, 23°C | Homo sapiens | methyl 11,12-dihydroxy-7-methoxyabieta-8(14),9(11),12-trien-20-oate | |
0.0012 | - |
pH 7.5, 23°C | Homo sapiens | N-[2-(dimethylamino)ethyl]-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-amide | |
0.0013 | - |
pH 7.5, 23°C | Homo sapiens | methyl 11,12-dihydroxy-7-[(2-hydroxyethyl)sulfanyl]abieta-8(14),9(11),12-trien-20-oate | |
0.0015 | - |
pH 7.5, 23°C | Homo sapiens | N'-acetyl-11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide | |
0.0022 | - |
pH 7.5, 23°C | Homo sapiens | (4bR,8aS)-4b-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol | |
0.0027 | - |
pH 7.5, 23°C | Homo sapiens | 11,12-dihydroxy-N-methylabieta-8(14),9(11),12-trien-20-amide | |
0.0027 | - |
pH 7.5, 23°C | Homo sapiens | 11,12-dihydroxy-N-[(pyridin-3-yl)methyl]abieta-8(14),9(11),12-trien-20-amide | |
0.0031 | - |
pH 7.5, 23°C | Homo sapiens | 2-[11,12-dihydroxy-20-oxoabieta-8(14),9(11),12-trien-20-yl]hydrazine-1-carboxamide | |
0.00603 | - |
pH 7.5, 23°C | Homo sapiens | N-benzyl-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-amide | |
0.0074 | - |
pH 7.5, 23°C | Homo sapiens | 4-[5-[(4aR,10aS)-5,6-dihydroxy-1,1-dimethyl-7-(propan-2-yl)-1,3,4,9,10,10a-hexahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]benzonitrile | |
0.0078 | - |
pH 7.5, 23°C | Homo sapiens | abieta-8(14),9(11),12-triene-11,12,20-triol | |
0.008 | - |
pH 7.5, 23°C | Homo sapiens | 11,12-dihydroxy-N-[3-(1H-imidazol-1-yl)propyl]abieta-8(14),9(11),12-trien-20-amide | |
0.008 | - |
pH 7.5, 23°C | Homo sapiens | N-[2-(dimethylamino)ethyl]-11,12-dihydroxy-7-oxoabieta-8(14),9(11),12-trien-20-amide | |
0.0086 | - |
pH 7.5, 23°C | Homo sapiens | methyl 7-ethoxy-11,12-dioxoabieta-8,13-dien-20-oate | |
0.0106 | - |
pH 7.5, 23°C | Homo sapiens | 12-hydroxy-11,20-epoxyabieta-8(14),9(11),12-trien-20-one | |
0.0125 | - |
pH 7.5, 23°C | Homo sapiens | methyl 7-(butylsulfanyl)-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate | |
0.0125 | - |
pH 7.5, 23°C | Homo sapiens | tert-butyl [(1R)-1-[5-[(4aR,10aS)-5,6-dihydroxy-1,1-dimethyl-9-oxo-7-(propan-2-yl)-1,3,4,9,10,10a-hexahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]ethyl]carbamate | |
0.0133 | - |
pH 7.5, 23°C | Homo sapiens | 11,12-dihydroxy-7,20-epoxyabieta-8,11,13-trien-20-one | |
0.0133 | - |
pH 7.5, 23°C | Homo sapiens | methyl 7-ethoxy-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate | |
0.0137 | - |
pH 7.5, 23°C | Homo sapiens | (4bR,8aS)-4b-[5-(4-bromophenyl)-1,3,4-oxadiazol-2-yl]-8,8-dimethyl-2-(propan-2-yl)-5,6,7,8,8a,9-hexahydrophenanthrene-3,4,10(4bH)-trione | |
0.0187 | - |
pH 7.5, 23°C | Homo sapiens | 7,20-epoxyabieta-8(14),9(11),12-triene-11,12-diol | |
0.0227 | - |
pH 7.5, 23°C | Homo sapiens | methyl 7-[(2-hydroxyethyl)sulfanyl]-11,12-dioxoabieta-8,13-dien-20-oate | |
0.0251 | - |
pH 7.5, 23°C | Homo sapiens | (4bR,8aS)-4b-[5-(4-bromophenyl)-1,3,4-oxadiazol-2-yl]-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol | |
0.02564 | - |
pH 7.5, 23°C | Homo sapiens | N-acetyl-S-((4aR,10aS)-5,6-dihydroxy-7-isopropyl-4a-(methoxycarbonyl)-1,1-dimethyl-1,2,3,4,4a,9,10,10a-octahydrophenanthren-9-yl)-L-cysteine | |
0.028 | - |
pH 7.5, 23°C | Homo sapiens | methyl 11,12-dihydroxy-7-(phenylsulfanyl)abieta-8(14),9(11),12-trien-20-oate | |
0.035 | - |
pH 7.5, 23°C | Homo sapiens | 11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide | |
0.0412 | - |
pH 7.5, 23°C | Homo sapiens | methyl 11,12-dihydroxy-7-oxoabieta-8(14),9(11),12-trien-20-oate | |
0.0563 | - |
pH 7.5, 23°C | Homo sapiens | methyl 11-[[tert-butyl(dimethyl)silyl]oxy]-12-hydroxyabieta-8(14),9(11),12-trien-20-oate |
General Information | Comment | Organism |
---|---|---|
drug target | the enzyme is a target for treating bone resorption diseases and some cancers | Homo sapiens |