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Compile Data Set for Download or QSAR

Found 153 hits Enz. Inhib. hit(s) with Target = 'Eukaryotic translation initiation factor 2-alpha kinase 4'   
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
GCN2(Kin.Dom.2 S808G)


(Homo sapiens)
BDBM31096
PNG
(CHEMBL290084 | Staurosporine | cid_451705)
Show SMILES CN[C@H]1C[C@@H]2O[C@](C)([C@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13
Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m0/s1
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Ambit Biosciences

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Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...


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Ligand-Target Pair
GCN2(Kin.Dom.2 S808G)


(Homo sapiens)
BDBM31094
PNG
(PKC-412 | cid_24202429)
Show SMILES CO[C@H]1[C@H](C[C@@H]2O[C@@]1(C)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13)N(C)C(=O)c1ccccc1
Show InChI InChI=1S/C35H30N4O4/c1-35-32(42-3)25(37(2)34(41)19-11-5-4-6-12-19)17-26(43-35)38-23-15-9-7-13-20(23)28-29-22(18-36-33(29)40)27-21-14-8-10-16-24(21)39(35)31(27)30(28)38/h4-16,25-26,32H,17-18H2,1-3H3,(H,36,40)/t25-,26-,32-,35+/m0/s1
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Ambit Biosciences

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Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...


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Ligand-Target Pair
GCN2(Kin.Dom.2 S808G)


(Homo sapiens)
BDBM31088
PNG
(1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-y...)
Show SMILES Cn1c(Nc2ccc(cc2)C(F)(F)F)nc2cc(Oc3ccnc(c3)-c3ncc([nH]3)C(F)(F)F)ccc12
Show InChI InChI=1S/C24H16F6N6O/c1-36-19-7-6-15(10-17(19)34-22(36)33-14-4-2-13(3-5-14)23(25,26)27)37-16-8-9-31-18(11-16)21-32-12-20(35-21)24(28,29)30/h2-12H,1H3,(H,32,35)(H,33,34)
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Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...


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Ligand-Target Pair
GCN2(Kin.Dom.2 S808G)


(Homo sapiens)
BDBM4814
PNG
(CHEMBL535 | N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fl...)
Show SMILES CCN(CC)CCNC(=O)c1c(C)[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c1C
Show InChI InChI=1S/C22H27FN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
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Ambit Biosciences

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Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...


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Ligand-Target Pair
GCN2(Kin.Dom.2 S808G)


(Homo sapiens)
BDBM25118
PNG
((3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,...)
Show SMILES CN1CCN(CC1)c1ccc2nc([nH]c2c1)-c1c(N)c2c(F)cccc2[nH]c1=O
Show InChI InChI=1S/C21H21FN6O/c1-27-7-9-28(10-8-27)12-5-6-14-16(11-12)25-20(24-14)18-19(23)17-13(22)3-2-4-15(17)26-21(18)29/h2-6,11H,7-10H2,1H3,(H,24,25)(H3,23,26,29)
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Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...


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Ligand-Target Pair
GCN2(Kin.Dom.2 S808G)


(Homo sapiens)
BDBM31090
PNG
((E)-N-[4-(3-chloro-4-fluoro-anilino)-3-cyano-7-eth...)
Show SMILES CCOc1cc2ncc(C#N)c(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)\C=C\CN(C)C
Show InChI InChI=1S/C24H23ClFN5O2/c1-4-33-22-12-20-17(11-21(22)30-23(32)6-5-9-31(2)3)24(15(13-27)14-28-20)29-16-7-8-19(26)18(25)10-16/h5-8,10-12,14H,4,9H2,1-3H3,(H,28,29)(H,30,32)/b6-5+
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Ambit Biosciences

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Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...


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Ligand-Target Pair
GCN2(Kin.Dom.2 S808G)


(Homo sapiens)
BDBM31095
PNG
(5-[(Z)-(5-fluoranyl-2-oxidanylidene-1H-indol-3-yli...)
Show SMILES Cc1[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c(C)c1C(=O)NC[C@H](O)CN1CCOCC1
Show InChI InChI=1S/C23H27FN4O4/c1-13-20(10-18-17-9-15(24)3-4-19(17)27-22(18)30)26-14(2)21(13)23(31)25-11-16(29)12-28-5-7-32-8-6-28/h3-4,9-10,16,26,29H,5-8,11-12H2,1-2H3,(H,25,31)(H,27,30)/b18-10-/t16-/m0/s1
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Ambit Biosciences

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Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...


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Ligand-Target Pair
GCN2(Kin.Dom.2 S808G)


(Homo sapiens)
BDBM13216
PNG
(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Show SMILES Cc1nc(Nc2ncc(s2)C(=O)Nc2c(C)cccc2Cl)cc(n1)N1CCN(CCO)CC1
Show InChI InChI=1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)
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Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...


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Ligand-Target Pair
GCN2(Kin.Dom.2 S808G)


(Homo sapiens)
BDBM13534
PNG
(CHEMBL572878 | N-[4-({4-[(3-methyl-1H-pyrazol-5-yl...)
Show SMILES CN1CCN(CC1)c1cc(Nc2cc(C)n[nH]2)nc(Sc2ccc(NC(=O)C3CC3)cc2)n1
Show InChI InChI=1S/C23H28N8OS/c1-15-13-20(29-28-15)25-19-14-21(31-11-9-30(2)10-12-31)27-23(26-19)33-18-7-5-17(6-8-18)24-22(32)16-3-4-16/h5-8,13-14,16H,3-4,9-12H2,1-2H3,(H,24,32)(H2,25,26,27,28,29)
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Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...


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Ligand-Target Pair
GCN2(Kin.Dom.2 S808G)


(Homo sapiens)
BDBM6866
PNG
(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Show SMILES Nc1nc(Nc2ccc(cc2)S(N)(=O)=O)nn1C(=O)c1c(F)cccc1F
Show InChI InChI=1S/C15H12F2N6O3S/c16-10-2-1-3-11(17)12(10)13(24)23-14(18)21-15(22-23)20-8-4-6-9(7-5-8)27(19,25)26/h1-7H,(H2,19,25,26)(H3,18,20,21,22)
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Ambit Biosciences

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Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...


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More data for this
Ligand-Target Pair
GCN2(Kin.Dom.2 S808G)


(Homo sapiens)
BDBM24773
PNG
(AMG 706 | AMG-706 | Motesanib | N-(3,3-dimethyl-1,...)
Show SMILES CC1(C)CNc2cc(NC(=O)c3cccnc3NCc3ccncc3)ccc12
Show InChI InChI=1S/C22H23N5O/c1-22(2)14-26-19-12-16(5-6-18(19)22)27-21(28)17-4-3-9-24-20(17)25-13-15-7-10-23-11-8-15/h3-12,26H,13-14H2,1-2H3,(H,24,25)(H,27,28)
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4.40E+6n/an/an/an/an/an/an/an/a



Ambit Biosciences

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Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...


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Ligand-Target Pair
GCN2(Kin.Dom.2 S808G)


(Homo sapiens)
BDBM5446
PNG
(CHEMBL553 | ERLOTINIB HYDROCHLORIDE | Erlotinib | ...)
Show SMILES COCCOc1cc2ncnc(Nc3cccc(c3)C#C)c2cc1OCCOC
Show InChI InChI=1S/C22H23N3O4/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25)
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Ambit Biosciences

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Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...


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Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072072
PNG
(CHEMBL3407849)
Show SMILES CNc1ncc2ccc(Oc3cc(ccc3C)C(=O)c3c(-c4ccccc4)n(C)n(-c4ccccc4)c3=O)cc2n1
Show InChI InChI=1S/C33H27N5O3/c1-21-14-15-23(18-28(21)41-26-17-16-24-20-35-33(34-2)36-27(24)19-26)31(39)29-30(22-10-6-4-7-11-22)37(3)38(32(29)40)25-12-8-5-9-13-25/h4-20H,1-3H3,(H,34,35,36)
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n/an/a 5n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072026
PNG
(CHEMBL3407851)
Show SMILES CNc1ncc2ccc(Oc3cc(ccc3Cl)C(=O)c3c(-c4ccccc4)n(C)n(-c4ccccc4)c3=O)cc2n1
Show InChI InChI=1S/C32H24ClN5O3/c1-34-32-35-19-22-13-15-24(18-26(22)36-32)41-27-17-21(14-16-25(27)33)30(39)28-29(20-9-5-3-6-10-20)37(2)38(31(28)40)23-11-7-4-8-12-23/h3-19H,1-2H3,(H,34,35,36)
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n/an/a 10n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50071957
PNG
(CHEMBL3407850)
Show SMILES CNc1ncc2ccc(Oc3cc(ccc3N)C(=O)c3c(-c4ccccc4)n(C)n(-c4ccccc4)c3=O)cc2n1
Show InChI InChI=1S/C32H26N6O3/c1-34-32-35-19-22-13-15-24(18-26(22)36-32)41-27-17-21(14-16-25(27)33)30(39)28-29(20-9-5-3-6-10-20)37(2)38(31(28)40)23-11-7-4-8-12-23/h3-19H,33H2,1-2H3,(H,34,35,36)
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n/an/a 12n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072027
PNG
(CHEMBL3407852)
Show SMILES CNc1ncc2c(F)cc(Oc3c(C)ccc(C(=O)c4c(-c5ccccc5)n(C)n(-c5ccccc5)c4=O)c3N)cc2n1
Show InChI InChI=1S/C33H27FN6O3/c1-19-14-15-23(28(35)31(19)43-22-16-25(34)24-18-37-33(36-2)38-26(24)17-22)30(41)27-29(20-10-6-4-7-11-20)39(3)40(32(27)42)21-12-8-5-9-13-21/h4-18H,35H2,1-3H3,(H,36,37,38)
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n/an/a 36n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072070
PNG
(CHEMBL3407504)
Show SMILES CNc1ncc2ccc(Oc3c(C)ccc(C(=O)c4c(-c5ccccc5)n(C)n(-c5ccccc5)c4=O)c3N)cc2n1
Show InChI InChI=1S/C33H28N6O3/c1-20-14-17-25(28(34)31(20)42-24-16-15-22-19-36-33(35-2)37-26(22)18-24)30(40)27-29(21-10-6-4-7-11-21)38(3)39(32(27)41)23-12-8-5-9-13-23/h4-19H,34H2,1-3H3,(H,35,36,37)
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n/an/a 42n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072028
PNG
(CHEMBL3407853)
Show SMILES CNc1ncc2c(Cl)cc(Oc3c(C)ccc(C(=O)c4c(-c5ccccc5)n(C)n(-c5ccccc5)c4=O)c3N)cc2n1
Show InChI InChI=1S/C33H27ClN6O3/c1-19-14-15-23(28(35)31(19)43-22-16-25(34)24-18-37-33(36-2)38-26(24)17-22)30(41)27-29(20-10-6-4-7-11-20)39(3)40(32(27)42)21-12-8-5-9-13-21/h4-18H,35H2,1-3H3,(H,36,37,38)
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Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072031
PNG
(CHEMBL3407857)
Show SMILES CNc1nc2ccc(cc2s1)-c1c(C)ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c1N
Show InChI InChI=1S/C32H27N5O2S/c1-19-14-16-23(28(33)26(19)21-15-17-24-25(18-21)40-32(34-2)35-24)30(38)27-29(20-10-6-4-7-11-20)36(3)37(31(27)39)22-12-8-5-9-13-22/h4-18H,33H2,1-3H3,(H,34,35)
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n/an/a 97n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072032
PNG
(CHEMBL3407858)
Show SMILES Cc1ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c(N)c1-c1ccc2nc(N)sc2c1
Show InChI InChI=1S/C31H25N5O2S/c1-18-13-15-22(27(32)25(18)20-14-16-23-24(17-20)39-31(33)34-23)29(37)26-28(19-9-5-3-6-10-19)35(2)36(30(26)38)21-11-7-4-8-12-21/h3-17H,32H2,1-2H3,(H2,33,34)
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Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072029
PNG
(CHEMBL3407854)
Show SMILES Cc1ncc2ccc(Oc3c(C)ccc(C(=O)c4c(-c5ccccc5)n(C)n(-c5ccccc5)c4=O)c3N)cc2n1
Show InChI InChI=1S/C33H27N5O3/c1-20-14-17-26(29(34)32(20)41-25-16-15-23-19-35-21(2)36-27(23)18-25)31(39)28-30(22-10-6-4-7-11-22)37(3)38(33(28)40)24-12-8-5-9-13-24/h4-19H,34H2,1-3H3
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Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072073
PNG
(CHEMBL3407848)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)c4c(-c5ccccc5)n(C)n(-c5ccccc5)c4=O)nc3)c2cc1OC
Show InChI InChI=1S/C33H27N5O5/c1-37-31(21-10-6-4-7-11-21)30(33(40)38(37)22-12-8-5-9-13-22)32(39)36-29-15-14-23(20-35-29)43-26-16-17-34-25-19-28(42-3)27(41-2)18-24(25)26/h4-20H,1-3H3,(H,35,36,39)
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n/an/a 290n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50011235
PNG
(CHEMBL3260333)
Show SMILES CCn1ccc(Nc2ncc3n(nnc3n2)-c2ccc(cc2)C(C)(C)OCCO)n1
Show InChI InChI=1S/C20H24N8O2/c1-4-27-10-9-17(25-27)22-19-21-13-16-18(23-19)24-26-28(16)15-7-5-14(6-8-15)20(2,3)30-12-11-29/h5-10,13,29H,4,11-12H2,1-3H3,(H,21,22,23,25)
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TBA

Assay Description
Inhibition of GCN2-mediated elF2alpha phosphorylation in human U2OS cells after 2 hrs by immunocytochemistry


Citation and Details
More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50011233
PNG
(CHEMBL3260331)
Show SMILES O[C@H]1CC[C@@H](CC1)n1ccc(Nc2ncc3n(nnc3n2)-c2ccc(Cl)c(F)c2)n1
Show InChI InChI=1S/C19H18ClFN8O/c20-14-6-3-12(9-15(14)21)29-16-10-22-19(24-18(16)25-27-29)23-17-7-8-28(26-17)11-1-4-13(30)5-2-11/h3,6-11,13,30H,1-2,4-5H2,(H,22,23,24,26)/t11-,13-
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TBA

Assay Description
Inhibition of GCN2-mediated elF2alpha phosphorylation in human U2OS cells after 2 hrs by immunocytochemistry


Citation and Details
More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50011232
PNG
(CHEMBL3260332)
Show SMILES CCOc1ccc(cc1)-n1nnc2nc(Nc3ccn(CCCC4CCNCC4)n3)ncc12
Show InChI InChI=1S/C23H29N9O/c1-2-33-19-7-5-18(6-8-19)32-20-16-25-23(27-22(20)28-30-32)26-21-11-15-31(29-21)14-3-4-17-9-12-24-13-10-17/h5-8,11,15-17,24H,2-4,9-10,12-14H2,1H3,(H,25,26,27,29)
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TBA

Assay Description
Inhibition of GCN2-mediated elF2alpha phosphorylation in human U2OS cells after 2 hrs by immunocytochemistry


Citation and Details
More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50011235
PNG
(CHEMBL3260333)
Show SMILES CCn1ccc(Nc2ncc3n(nnc3n2)-c2ccc(cc2)C(C)(C)OCCO)n1
Show InChI InChI=1S/C20H24N8O2/c1-4-27-10-9-17(25-27)22-19-21-13-16-18(23-19)24-26-28(16)15-7-5-14(6-8-15)20(2,3)30-12-11-29/h5-10,13,29H,4,11-12H2,1-3H3,(H,21,22,23,25)
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TBA

Assay Description
Inhibition of GCN2 (unknown origin) using GFP-elF2a as substrate preincubated with substrate for 20 mins measured after 90 mins by Lanthascreen assay


Citation and Details
More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50011234
PNG
(CHEMBL3260330)
Show SMILES C1CC(CCO1)n1ccc(Nc2ncc3n(nnc3n2)-c2ccc3cn[nH]c3c2)n1
Show InChI InChI=1S/C19H18N10O/c1-2-14(9-15-12(1)10-21-24-15)29-16-11-20-19(23-18(16)25-27-29)22-17-3-6-28(26-17)13-4-7-30-8-5-13/h1-3,6,9-11,13H,4-5,7-8H2,(H,21,24)(H,20,22,23,26)
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TBA

Assay Description
Inhibition of GCN2 (unknown origin) using GFP-elF2a as substrate preincubated with substrate for 20 mins measured after 90 mins by Lanthascreen assay


Citation and Details
More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50011234
PNG
(CHEMBL3260330)
Show SMILES C1CC(CCO1)n1ccc(Nc2ncc3n(nnc3n2)-c2ccc3cn[nH]c3c2)n1
Show InChI InChI=1S/C19H18N10O/c1-2-14(9-15-12(1)10-21-24-15)29-16-11-20-19(23-18(16)25-27-29)22-17-3-6-28(26-17)13-4-7-30-8-5-13/h1-3,6,9-11,13H,4-5,7-8H2,(H,21,24)(H,20,22,23,26)
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TBA

Assay Description
Inhibition of GCN2-mediated elF2alpha phosphorylation in human U2OS cells after 2 hrs by immunocytochemistry


Citation and Details
More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50011233
PNG
(CHEMBL3260331)
Show SMILES O[C@H]1CC[C@@H](CC1)n1ccc(Nc2ncc3n(nnc3n2)-c2ccc(Cl)c(F)c2)n1
Show InChI InChI=1S/C19H18ClFN8O/c20-14-6-3-12(9-15(14)21)29-16-10-22-19(24-18(16)25-27-29)23-17-7-8-28(26-17)11-1-4-13(30)5-2-11/h3,6-11,13,30H,1-2,4-5H2,(H,22,23,24,26)/t11-,13-
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TBA

Assay Description
Inhibition of GCN2 (unknown origin) using GFP-elF2a as substrate preincubated with substrate for 20 mins measured after 90 mins by Lanthascreen assay


Citation and Details
More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50011232
PNG
(CHEMBL3260332)
Show SMILES CCOc1ccc(cc1)-n1nnc2nc(Nc3ccn(CCCC4CCNCC4)n3)ncc12
Show InChI InChI=1S/C23H29N9O/c1-2-33-19-7-5-18(6-8-19)32-20-16-25-23(27-22(20)28-30-32)26-21-11-15-31(29-21)14-3-4-17-9-12-24-13-10-17/h5-8,11,15-17,24H,2-4,9-10,12-14H2,1H3,(H,25,26,27,29)
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n/an/a<300n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of GCN2 (unknown origin) using GFP-elF2a as substrate preincubated with substrate for 20 mins measured after 90 mins by Lanthascreen assay


Citation and Details
More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072033
PNG
(CHEMBL3407859)
Show SMILES Cc1ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c(N)c1-c1ccc2nc(CF)sc2c1
Show InChI InChI=1S/C32H25FN4O2S/c1-19-13-15-23(29(34)27(19)21-14-16-24-25(17-21)40-26(18-33)35-24)31(38)28-30(20-9-5-3-6-10-20)36(2)37(32(28)39)22-11-7-4-8-12-22/h3-17H,18,34H2,1-2H3
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Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072074
PNG
(CHEMBL3407847)
Show SMILES CNc1ncc2cc(ccc2n1)-c1c(C)ccc(C(=O)Nc2ccc(OC)c(c2)C(F)(F)F)c1N
Show InChI InChI=1S/C25H22F3N5O2/c1-13-4-7-17(23(34)32-16-6-9-20(35-3)18(11-16)25(26,27)28)22(29)21(13)14-5-8-19-15(10-14)12-31-24(30-2)33-19/h4-12H,29H2,1-3H3,(H,32,34)(H,30,31,33)
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Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50096279
PNG
(CHEMBL3577124)
Show SMILES CNc1ncc2cc(c(C)nc2n1)-c1cc(NC(=O)NCCC(C)(C)C)c(F)cc1C
Show InChI InChI=1S/C18H13N3O5/c22-14(23)5-4-10-8-21-13-7-12-9(6-15(24)25)2-1-3-11(12)16(13)20-18(26)17(21)19-10/h1-5,8H,6-7H2,(H,20,26)(H,22,23)(H,24,25)/b5-4+
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n/an/a 450n/an/an/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Competitive binding affinity to GCN2 in human A375 cells after 15 mins in presence of ATP analogue


J Med Chem 58: 4165-79 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072034
PNG
(CHEMBL3407860)
Show SMILES Cc1ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c(N)c1-c1ccc2nc(sc2c1)C(F)F
Show InChI InChI=1S/C32H24F2N4O2S/c1-18-13-15-22(27(35)25(18)20-14-16-23-24(17-20)41-31(36-23)30(33)34)29(39)26-28(19-9-5-3-6-10-19)37(2)38(32(26)40)21-11-7-4-8-12-21/h3-17,30H,35H2,1-2H3
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Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50442162
PNG
(CHEMBL2441342)
Show SMILES Cn1cc(-c2ccc3N(CCc3c2F)C(=O)Cc2cccc(n2)C(F)(F)F)c2c(N)ncnc12
Show InChI InChI=1S/C23H18F4N6O/c1-32-10-15(19-21(28)29-11-30-22(19)32)13-5-6-16-14(20(13)24)7-8-33(16)18(34)9-12-3-2-4-17(31-12)23(25,26)27/h2-6,10-11H,7-9H2,1H3,(H2,28,29,30)
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n/an/a 776n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of GCN2 (unknown origin) assessed as EIF2AK4 phosphorylation


Citation and Details
More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072030
PNG
(CHEMBL3407856)
Show SMILES Cc1nc2ccc(cc2s1)-c1c(C)ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c1N
Show InChI InChI=1S/C32H26N4O2S/c1-19-14-16-24(29(33)27(19)22-15-17-25-26(18-22)39-20(2)34-25)31(37)28-30(21-10-6-4-7-11-21)35(3)36(32(28)38)23-12-8-5-9-13-23/h4-18H,33H2,1-3H3
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n/an/a 1.40E+3n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50442166
PNG
(CHEMBL2441340)
Show SMILES Cc1cccc(CC(=O)N2CCc3c2ccc(-c2cn(C)c4ncnc(N)c24)c3F)n1
Show InChI InChI=1S/C23H21FN6O/c1-13-4-3-5-14(28-13)10-19(31)30-9-8-16-18(30)7-6-15(21(16)24)17-11-29(2)23-20(17)22(25)26-12-27-23/h3-7,11-12H,8-10H2,1-2H3,(H2,25,26,27)
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n/an/a 3.39E+3n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of GCN2 (unknown origin) assessed as EIF2AK4 phosphorylation


Citation and Details
More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072075
PNG
(CHEMBL3407846)
Show SMILES Cn1cc(-c2ccc3N(CC(=O)c4cc(F)cc(c4)C(F)(F)F)CCc3c2)c2c(N)ncnc12
Show InChI InChI=1S/C24H19F4N5O/c1-32-10-18(21-22(29)30-12-31-23(21)32)13-2-3-19-14(6-13)4-5-33(19)11-20(34)15-7-16(24(26,27)28)9-17(25)8-15/h2-3,6-10,12H,4-5,11H2,1H3,(H2,29,30,31)
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n/an/a 3.90E+3n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072036
PNG
(CHEMBL3407862)
Show SMILES Cc1ccc2cc(ccc2n1)-c1c(C)ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c1N
Show InChI InChI=1S/C34H28N4O2/c1-21-14-18-27(31(35)29(21)25-17-19-28-24(20-25)16-15-22(2)36-28)33(39)30-32(23-10-6-4-7-11-23)37(3)38(34(30)40)26-12-8-5-9-13-26/h4-20H,35H2,1-3H3
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n/an/a 7.30E+3n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072071
PNG
(CHEMBL3407855)
Show SMILES Cc1nc2cc(ccc2s1)-c1c(C)ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c1N
Show InChI InChI=1S/C32H26N4O2S/c1-19-14-16-24(29(33)27(19)22-15-17-26-25(18-22)34-20(2)39-26)31(37)28-30(21-10-6-4-7-11-21)35(3)36(32(28)38)23-12-8-5-9-13-23/h4-18H,33H2,1-3H3
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n/an/a>1.00E+4n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50401152
PNG
(CHEMBL2205766)
Show SMILES CC(C)(C)NS(=O)(=O)c1cncc(c1)-c1ccn2nc(N)nc2c1
Show InChI InChI=1S/C15H18N6O2S/c1-15(2,3)20-24(22,23)12-6-11(8-17-9-12)10-4-5-21-13(7-10)18-14(16)19-21/h4-9,20H,1-3H3,(H2,16,19)
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n/an/a<1.00E+4n/an/an/an/an/an/a



Cellzome Ltd

Curated by ChEMBL


Assay Description
Inhibition of EIF2AK4


Bioorg Med Chem Lett 22: 4613-8 (2012)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072038
PNG
(CHEMBL3407863)
Show SMILES Cc1nc(N)c2c(cn(C)c2n1)-c1ccc2N(CC(=O)c3cc(F)cc(c3)C(F)(F)F)CCc2c1
Show InChI InChI=1S/C25H21F4N5O/c1-13-31-23(30)22-19(11-33(2)24(22)32-13)14-3-4-20-15(7-14)5-6-34(20)12-21(35)16-8-17(25(27,28)29)10-18(26)9-16/h3-4,7-11H,5-6,12H2,1-2H3,(H2,30,31,32)
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Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50072035
PNG
(CHEMBL3407861)
Show SMILES Cc1ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c(N)c1-c1ccc2nc(sc2c1)C(F)(F)F
Show InChI InChI=1S/C32H23F3N4O2S/c1-18-13-15-22(27(36)25(18)20-14-16-23-24(17-20)42-31(37-23)32(33,34)35)29(40)26-28(19-9-5-3-6-10-19)38(2)39(30(26)41)21-11-7-4-8-12-21/h3-17H,36H2,1-2H3
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n/an/a>5.00E+4n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...


J Med Chem 58: 1426-41 (2015)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50355499
PNG
(CHEMBL1908395 | CHEMBL1908842)
Show SMILES CN(C)CC(=O)N1CCC(CC1)c1ccc(NC(=O)c2ncc([nH]2)C#N)c(c1)C1=CCCCC1
Show InChI InChI=1S/C26H32N6O2/c1-31(2)17-24(33)32-12-10-18(11-13-32)20-8-9-23(22(14-20)19-6-4-3-5-7-19)30-26(34)25-28-16-21(15-27)29-25/h6,8-9,14,16,18H,3-5,7,10-13,17H2,1-2H3,(H,28,29)(H,30,34)
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n/an/an/a 81n/an/an/an/an/a



Ambit Biosciences

Curated by ChEMBL


Assay Description
Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain


Nat Biotechnol 29: 1046-51 (2011)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50355494
PNG
(CHEMBL1908396)
Show SMILES COc1cc(Oc2ccnc3cc(OC)c(OC)cc23)ccc1NC(=O)NC(C)c1nccs1
Show InChI InChI=1S/C24H24N4O5S/c1-14(23-26-9-10-34-23)27-24(29)28-17-6-5-15(11-20(17)30-2)33-19-7-8-25-18-13-22(32-4)21(31-3)12-16(18)19/h5-14H,1-4H3,(H2,27,28,29)
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Ambit Biosciences

Curated by ChEMBL


Assay Description
Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain


Nat Biotechnol 29: 1046-51 (2011)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50355496
PNG
(CHEMBL1908397)
Show SMILES O=C(N1CCNCC1)c1ccc(\C=C\c2n[nH]c3ccccc23)cc1
Show InChI InChI=1S/C20H20N4O/c25-20(24-13-11-21-12-14-24)16-8-5-15(6-9-16)7-10-19-17-3-1-2-4-18(17)22-23-19/h1-10,21H,11-14H2,(H,22,23)/b10-7+
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n/an/an/a 330n/an/an/an/an/a



Ambit Biosciences

Curated by ChEMBL


Assay Description
Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain


Nat Biotechnol 29: 1046-51 (2011)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM13535
PNG
(4-[6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin...)
Show SMILES COc1cc2c(ncnc2cc1OCCCN1CCCCC1)N1CCN(CC1)C(=O)Nc1ccc(OC(C)C)cc1
Show InChI InChI=1S/C31H42N6O4/c1-23(2)41-25-10-8-24(9-11-25)34-31(38)37-17-15-36(16-18-37)30-26-20-28(39-3)29(21-27(26)32-22-33-30)40-19-7-14-35-12-5-4-6-13-35/h8-11,20-23H,4-7,12-19H2,1-3H3,(H,34,38)
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n/an/an/a>1.00E+4n/an/an/an/an/a



Ambit Biosciences

Curated by ChEMBL


Assay Description
Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain


Nat Biotechnol 29: 1046-51 (2011)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM50132260
PNG
(2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmetho...)
Show SMILES Fc1ccc(C(=O)NOCC2CC2)c(Nc2ccc(I)cc2Cl)c1F
Show InChI InChI=1S/C17H14ClF2IN2O2/c18-12-7-10(21)3-6-14(12)22-16-11(4-5-13(19)15(16)20)17(24)23-25-8-9-1-2-9/h3-7,9,22H,1-2,8H2,(H,23,24)
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Ambit Biosciences

Curated by ChEMBL


Assay Description
Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain


Nat Biotechnol 29: 1046-51 (2011)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM60665
PNG
(BDBM50249542 | US9145414, R406 | US9212178, R406)
Show SMILES COc1cc(Nc2ncc(F)c(Nc3ccc4OC(C)(C)C(=O)Nc4n3)n2)cc(OC)c1OC
Show InChI InChI=1S/C22H23FN6O5/c1-22(2)20(30)28-19-13(34-22)6-7-16(27-19)26-18-12(23)10-24-21(29-18)25-11-8-14(31-3)17(33-5)15(9-11)32-4/h6-10H,1-5H3,(H3,24,25,26,27,28,29,30)
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n/an/an/a 3.30n/an/an/an/an/a



Ambit Biosciences

Curated by ChEMBL


Assay Description
Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain


Nat Biotechnol 29: 1046-51 (2011)

More data for this
Ligand-Target Pair
Eukaryotic translation initiation factor 2-alpha kinase 4


(Homo sapiens)
BDBM13533
PNG
(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Show SMILES Cc1ccc(cc1)-n1nc(cc1NC(=O)Nc1ccc(OCCN2CCOCC2)c2ccccc12)C(C)(C)C
Show InChI InChI=1S/C31H37N5O3/c1-22-9-11-23(12-10-22)36-29(21-28(34-36)31(2,3)4)33-30(37)32-26-13-14-27(25-8-6-5-7-24(25)26)39-20-17-35-15-18-38-19-16-35/h5-14,21H,15-20H2,1-4H3,(H2,32,33,37)
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Ambit Biosciences

Curated by ChEMBL


Assay Description
Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain


Nat Biotechnol 29: 1046-51 (2011)

More data for this
Ligand-Target Pair
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