BindingDB logo
myBDB logout

Patent code US9765040

Compile Data Set for Download or QSAR
Found 15 hits of Enzyme Inhibition Constant Data   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340548
PNG
(US9765040, Compound 1)
Show SMILES Cn1c(nnc1C(C)(C)Oc1c(F)cc(F)cc1F)-c1ccc(F)cc1Br
Show InChI InChI=1S/C18H14BrF4N3O/c1-18(2,27-15-13(22)7-10(21)8-14(15)23)17-25-24-16(26(17)3)11-5-4-9(20)6-12(11)19/h4-8H,1-3H3
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 35n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340791
PNG
(US9765040, Compound 4)
Show SMILES Cn1c(nnc1C(C)(C)Oc1c(F)cc(Cl)cc1F)-c1ccccc1Cl
Show InChI InChI=1S/C18H15Cl2F2N3O/c1-18(2,26-15-13(21)8-10(19)9-14(15)22)17-24-23-16(25(17)3)11-6-4-5-7-12(11)20/h4-9H,1-3H3
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 32n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340798
PNG
(US9765040, Compound 9)
Show SMILES CC(C)n1c(nnc1C(C)(C)Oc1c(F)cc(F)cc1F)-c1ccc(cc1)C(N)=O
Show InChI InChI=1S/C21H21F3N4O2/c1-11(2)28-19(13-7-5-12(6-8-13)18(25)29)26-27-20(28)21(3,4)30-17-15(23)9-14(22)10-16(17)24/h5-11H,1-4H3,(H2,25,29)
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 26n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340810
PNG
(US9765040, Compound 12)
Show SMILES Cn1c(nnc1C(C)(C)Oc1c(F)cc(F)cc1F)-c1ccc(cc1F)C(N)=O
Show InChI InChI=1S/C19H16F4N4O2/c1-19(2,29-15-13(22)7-10(20)8-14(15)23)18-26-25-17(27(18)3)11-5-4-9(16(24)28)6-12(11)21/h4-8H,1-3H3,(H2,24,28)
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 182n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340799
PNG
(US9765040, Compound 10)
Show SMILES Cn1c(nnc1C(C)(C)Oc1c(F)cc(Cl)cc1F)-c1ccc(cc1F)C(N)=O
Show InChI InChI=1S/C19H16ClF3N4O2/c1-19(2,29-15-13(22)7-10(20)8-14(15)23)18-26-25-17(27(18)3)11-5-4-9(16(24)28)6-12(11)21/h4-8H,1-3H3,(H2,24,28)
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 135n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340814
PNG
(US9765040, Compound 13)
Show SMILES CC(C)n1c(nnc1C(C)(C)Oc1c(F)cc(Cl)cc1F)-c1ccc(cc1)C(N)=O
Show InChI InChI=1S/C21H21ClF2N4O2/c1-11(2)28-19(13-7-5-12(6-8-13)18(25)29)26-27-20(28)21(3,4)30-17-15(23)9-14(22)10-16(17)24/h5-11H,1-4H3,(H2,25,29)
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 68n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340792
PNG
(US9765040, Compound 5)
Show SMILES Cn1c(nnc1C(C)(C)Oc1c(F)cc(Cl)cc1F)-c1ccc(F)cc1Cl
Show InChI InChI=1S/C18H14Cl2F3N3O/c1-18(2,27-15-13(22)6-9(19)7-14(15)23)17-25-24-16(26(17)3)11-5-4-10(21)8-12(11)20/h4-8H,1-3H3
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 263n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340796
PNG
(US9765040, Compound 7)
Show SMILES Cn1c(nnc1C(C)(C)Oc1c(F)cc(F)cc1F)-c1c[nH]nc1C(F)(F)F
Show InChI InChI=1S/C16H13F6N5O/c1-15(2,28-11-9(18)4-7(17)5-10(11)19)14-26-25-13(27(14)3)8-6-23-24-12(8)16(20,21)22/h4-6H,1-3H3,(H,23,24)
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 32n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340822
PNG
(US9765040, Compound 14)
Show SMILES CC(C)(Oc1ccc(F)cc1F)c1nnc(-c2ccc(cc2Cl)C(N)=O)n1C1CC1
Show InChI InChI=1S/C21H19ClF2N4O2/c1-21(2,30-17-8-4-12(23)10-16(17)24)20-27-26-19(28(20)13-5-6-13)14-7-3-11(18(25)29)9-15(14)22/h3-4,7-10,13H,5-6H2,1-2H3,(H2,25,29)
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 16n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340790
PNG
(US9765040, Compound 3)
Show SMILES Cn1c(nnc1C(C)(C)Oc1c(F)cc(F)cc1F)-c1ccccc1Cl
Show InChI InChI=1S/C18H15ClF3N3O/c1-18(2,26-15-13(21)8-10(20)9-14(15)22)17-24-23-16(25(17)3)11-6-4-5-7-12(11)19/h4-9H,1-3H3
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 24n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340797
PNG
(US9765040, Compound 8)
Show SMILES CCn1c(nnc1C(C)(C)Oc1c(F)cc(Cl)cc1F)-c1ccc(cc1)C(N)=O
Show InChI InChI=1S/C20H19ClF2N4O2/c1-4-27-18(12-7-5-11(6-8-12)17(24)28)25-26-19(27)20(2,3)29-16-14(22)9-13(21)10-15(16)23/h5-10H,4H2,1-3H3,(H2,24,28)
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 70n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340823
PNG
(US9765040, Compound 15)
Show SMILES CC(C)n1c(nnc1C(C)(C)Oc1c(F)cc(F)cc1F)-c1ccc(cc1F)C(N)=O
Show InChI InChI=1S/C21H20F4N4O2/c1-10(2)29-19(13-6-5-11(18(26)30)7-14(13)23)27-28-20(29)21(3,4)31-17-15(24)8-12(22)9-16(17)25/h5-10H,1-4H3,(H2,26,30)
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 23n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340642
PNG
(US9765040, Compound 2)
Show SMILES Cn1c(nnc1C(C)(C)Oc1c(F)cc(F)cc1F)-c1ccc(F)cc1Cl
Show InChI InChI=1S/C18H14ClF4N3O/c1-18(2,27-15-13(22)7-10(21)8-14(15)23)17-25-24-16(26(17)3)11-5-4-9(20)6-12(11)19/h4-8H,1-3H3
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 52n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340803
PNG
(US9765040, Compound 11)
Show SMILES CC(C)(Oc1ccc(F)cc1F)c1nnc(-c2ccc(cc2F)C(N)=O)n1C1CC1
Show InChI InChI=1S/C21H19F3N4O2/c1-21(2,30-17-8-4-12(22)10-16(17)24)20-27-26-19(28(20)13-5-6-13)14-7-3-11(18(25)29)9-15(14)23/h3-4,7-10,13H,5-6H2,1-2H3,(H2,25,29)
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 64n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1)


(Rattus norvegicus (rat))
BDBM340793
PNG
(US9765040, Compound 6)
Show SMILES Cn1c(nnc1C(C)(C)Oc1c(F)cc(F)cc1F)-c1ccccc1F
Show InChI InChI=1S/C18H15F4N3O/c1-18(2,26-15-13(21)8-10(19)9-14(15)22)17-24-23-16(25(17)3)11-6-4-5-7-12(11)20/h4-9H,1-3H3
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 322n/an/an/an/an/an/a



Astellas Pharma Inc.

US Patent


Assay Description
The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384...


US Patent US9765040 (2017)

More data for this
Ligand-Target Pair
* indicates data uncertainty>20%