General Information of the Protein
Protein ID
PT01533
Protein Name
Mitogen-activated protein kinase kinase kinase 5
Secondarily
Protein Name
Apoptosis signal-regulating kinase 1
MAPK/ERK kinase kinase 5
Gene Name
MAP3K5
Secondarily
Gene Name
ASK1
MAPKKK5
MEKK5
Sequence
MSTEADEGITFSVPPFAPSGFCTIPEGGICRRGGAAAVGEGEEHQLPPPPPGSFWNVESAAAPGIGCPAATSSSSATRGRGSSVGGGSRRTTVAYVINEASQGQLVVAESEALQSLREACETVGATLETLHFGKLDFGETTVLDRFYNADIAVVEMSDAFRQPSLFYHLGVRESFSMANNIILYCDTNSDSLQSLKEIICQKNTMCTGNYTFVPYMITPHNKVYCCDSSFMKGLTELMQPNFELLLGPICLPLVDRFIQLLKVAQASSSQYFRESILNDIRKARNLYTGKELAAELARIRQRVDNIEVLTADIVINLLLSYRDIQDYDSIVKLVETLEKLPTFDLASHHHVKFHYAFALNRRNLPGDRAKALDIMIPMVQSEGQVASDMYCLVGRIYKDMFLDSNFTDTESRDHGASWFKKAFESEPTLQSGINYAVLLLAAGHQFESSFELRKVGVKLSSLLGKKGNLEKLQSYWEVGFFLGASVLANDHMRVIQASEKLFKLKTPAWYLKSIVETILIYKHFVKLTTEQPVAKQELVDFWMDFLVEATKTDVTVVRFPVLILEPTKIYQPSYLSINNEVEEKTISIWHVLPDDKKGIHEWNFSASSVRGVSISKFEERCCFLYVLHNSDDFQIYFCTELHCKKFFEMVNTITEEKGRSTEEGDCESDLLEYDYEYDENGDRVVLGKGTYGIVYAGRDLSNQVRIAIKEIPERDSRYSQPLHEEIALHKHLKHKNIVQYLGSFSENGFIKIFMEQVPGGSLSALLRSKWGPLKDNEQTIGFYTKQILEGLKYLHDNQIVHRDIKGDNVLINTYSGVLKISDFGTSKRLAGINPCTETFTGTLQYMAPEIIDKGPRGYGKAADIWSLGCTIIEMATGKPPFYELGEPQAAMFKVGMFKVHPEIPESMSAEAKAFILKCFEPDPDKRACANDLLVDEFLKVSSKKKKTQPKLSALSAGSNEYLRSISLPVPVLVEDTSSSSEYGSVSPDTELKVDPFSFKTRAKSCGERDVKGIRTLFLGIPDENFEDHSAPPSPEEKDSGFFMLRKDSERRATLHRILTEDQDKIVRNLMESLAQGAEEPKLKWEHITTLIASLREFVRSTDRKIIATTLSKLKLELDFDSHGISQVQVVLFGFQDAVNKVLRNHNIKPHWMFALDSIIRKAVQTAITILVPELRPHFSLASESDTADQEDLDVEDDHEEQPSNQTVRRPQAVIEDAVATSGVSTLSSTVSHDSQSAHRSLNVQLGRMKIETNRLLEELVRKEKELQALLHRAIEEKDQEIKHLKLKSQPIEIPELPVFHLNSSGTNTEDSELTDWLRVNGADEDTISRFLAEDYTLLDVLYYVTRDDLKCLRLRGGMLCTLWKAIIDFRNKQT
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
STE protein kinase group
>
STE protein kinase STE11 family
Function
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. Plays an important role in the cascades of cellular responses evoked by changes in the environment. Mediates signaling for determination of cell fate such as differentiation and survival. Plays a crucial role in the apoptosis signal transduction pathway through mitochondria-dependent caspase activation. MAP3K5/ASK1 is required for the innate immune response, which is essential for host defense against a wide range of pathogens. Mediates signal transduction of various stressors like oxidative stress as well as by receptor-mediated inflammatory signals, such as the tumor necrosis factor (TNF) or lipopolysaccharide (LPS). Once activated, acts as an upstream activator of the MKK/JNK signal transduction cascade and the p38 MAPK signal transduction cascade through the phosphorylation and activation of several MAP kinase kinases like MAP2K4/SEK1, MAP2K3/MKK3, MAP2K6/MKK6 and MAP2K7/MKK7. These MAP2Ks in turn activate p38 MAPKs and c-jun N-terminal kinases (JNKs). Both p38 MAPK and JNKs control the transcription factors activator protein-1 (AP-1).
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Uniprot ID
Primary ID:
Q99683

Secondarily ID:
A6NIA0
B4DGB2
Q5THN3
Q99461
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Ensembl ID
ENSG00000197442
HGNC ID
HGNC:6857
Subcellular Location
Cytoplasm
Endoplasmic reticulum
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: CL000927 , 293/AP1-luc
Compound ID Compound Name Compound Formula
CP0478996
4-methoxy-6-methyl-3-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]benzene-1,3-dicarboxamide
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C20H22N6O3
 1
1
IC50 = 28 nM
   TI
   LI
   LO
   TS
CP0559576
5-(ethylsulfonylamino)-2-methoxy-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]benzamide
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C20H24N6O4S
 1
1
IC50 = 41 nM
   TI
   LI
   LO
   TS
CP0446241
2-methoxy-4-methyl-5-methylsulfonyl-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]benzamide
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C20H23N5O4S
 1
1
IC50 = 73 nM
   TI
   LI
   LO
   TS
CP0536528
2-methoxy-4-methyl-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]-5-sulfamoylbenzamide
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C19H22N6O4S
 1
1
IC50 = 84 nM
   TI
   LI
   LO
   TS
CP0458126
4-methoxy-3-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]benzene-1,3-dicarboxamide
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C19H20N6O3
 1
1
IC50 = 94 nM
   TI
   LI
   LO
   TS
CP0446235
2-methoxy-5-methylsulfonyl-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]benzamide
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C19H21N5O4S
 1
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
CP0559567
4-methoxy-1-N-methyl-3-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]benzene-1,3-dicarboxamide
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C20H22N6O3
 1
1
IC50 = 272 nM
   TI
   LI
   LO
   TS
CP0401740
2-methoxy-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]-5-sulfamoylbenzamide
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C18H20N6O4S
 1
1
IC50 = 736 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0176880
3-methoxy-1-methyl-N-[6-[4-[1-(trifluoromethyl)cyclopropyl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyrazole-4-carboxamide
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C17H16F3N7O2
 1
1 IC50 = 1 nM
CP0416385
1-[5-(dimethylamino)pyridin-3-yl]-3-methoxy-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]pyrazole-4-carboxamide
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C22H25N9O2
 1
1 IC50 = 1.9 nM
CP0176881
1-ethyl-3-methoxy-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyrazole-4-carboxamide
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C17H18F3N7O2
 1
1 IC50 = 2 nM
CP0419295
1-(cyclopropylmethyl)-3-methoxy-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyrazole-4-carboxamide
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C19H20F3N7O2
 1
1 IC50 = 2 nM
CP0555055
3-methoxy-1-(2-methoxyethyl)-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyrazole-4-carboxamide
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C18H20F3N7O3
 1
1 IC50 = 2 nM
CP0565299
N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]quinoline-8-carboxamide
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C20H15F3N6O
 1
1 IC50 = 2 nM
CP0354745
3-methoxy-1-methyl-N-[6-(3-propan-2-ylimidazol-4-yl)pyridin-2-yl]pyrazole-4-carboxamide
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C17H20N6O2
 1
1 IC50 = 2.4 nM
CP0217203
GS-4997
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C24H24FN7O
 7
1 IC50 = 3 nM
2 IC50 = 5 nM
3 IC50 = 5.5 nM
4 IC50 = 5.9 nM
5 IC50 = 6 nM
6 IC50 = 12.9 nM
7 IC50 = 24.4 nM
CP0444649
3-methoxy-1-pyrazin-2-yl-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyrazole-4-carboxamide
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C19H16F3N9O2
 1
1 IC50 = 3 nM
CP0546434
3-methoxy-1-(2,2,2-trifluoroethyl)-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyrazole-4-carboxamide
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C17H15F6N7O2
 1
1 IC50 = 3 nM
CP0546435
2-methoxy-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]benzamide
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C18H16F3N5O2
 1
1 IC50 = 3 nM
CP0555056
2-methoxy-5-methyl-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyridine-3-carboxamide
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C18H17F3N6O2
 1
1 IC50 = 3 nM
CP0561697
3-methoxy-1-pyridazin-3-yl-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyrazole-4-carboxamide
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C19H16F3N9O2
 1
1 IC50 = 3 nM
CP0564283
3-methoxy-1-methyl-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyrazole-4-carboxamide
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C16H16F3N7O2
 1
1 IC50 = 3 nM
CP0570837
N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]quinoxaline-5-carboxamide
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C19H14F3N7O
 1
1 IC50 = 3 nM
CP0368689
3-methoxy-1-methyl-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]pyrazole-4-carboxamide
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C16H19N7O2
 2
1 IC50 = 3.9 nM
2 IC50 = 6 nM
CP0326338
15-(4-methylimidazol-1-yl)-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12(17),13,15,20,22-octaen-18-one
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C22H21N7O2
 1
1 IC50 = 4 nM
CP0402031
(7S)-7-methyl-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12,14,16,20,22-octaen-18-one
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C19H19N5O2
 1
1 IC50 = 4 nM
CP0368691
1-ethyl-3-methoxy-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]pyrazole-4-carboxamide
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C17H21N7O2
 1
1 IC50 = 4.1 nM
CP0519313
15-(1-methylpyrazol-4-yl)-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12(17),13,15,20,22-octaen-18-one
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C22H21N7O2
 1
1 IC50 = 5 nM
CP0561696
3-methoxy-1-methyl-N-[6-[4-[(3R)-oxolan-3-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyrazole-4-carboxamide
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C17H19N7O3
 1
1 IC50 = 5 nM
CP0569729
N-[6-[4-(2,2-difluorocyclobutyl)-1,2,4-triazol-3-yl]pyridin-2-yl]-3-methoxy-1-methylpyrazole-4-carboxamide
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C17H17F2N7O2
 1
1 IC50 = 5 nM
CP0163184
3-methoxy-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]-1-pyridin-3-ylpyrazole-4-carboxamide
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C20H20N8O2
 1
1 IC50 = 5.3 nM
CP0354744
1-(5-cyclopropylpyridin-3-yl)-3-methoxy-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]pyrazole-4-carboxamide
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C23H24N8O2
 1
1 IC50 = 5.6 nM
CP0402034
15-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12(17),13,15,20,22-octaen-18-one
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C25H28N8O2
 1
1 IC50 = 6 nM
CP0355865
N-[6-[4-[(2S)-1,1-difluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]-3-methoxy-1-methylpyrazole-4-carboxamide
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C16H17F2N7O2
 1
1 IC50 = 6 nM
CP0356980
N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-4-oxo-1-propan-2-ylquinoline-3-carboxamide
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C30H27N3O5
 2
1 IC50 = 6 nM
2 IC50 = 9 nM
CP0125432
(7S)-7,14-dimethyl-11-oxa-3,4,6,13,14,18,23-heptazatetracyclo[17.3.1.02,6.012,16]tricosa-1(23),2,4,12,15,19,21-heptaen-17-one
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C17H19N7O2
 1
1 IC50 = 6.8 nM
CP0125694
1-(cyclopropylmethyl)-3-methoxy-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]pyrazole-4-carboxamide
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C19H23N7O2
 1
1 IC50 = 6.9 nM
CP0402033
(7S)-14-fluoro-7-methyl-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12(17),13,15,20,22-octaen-18-one
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C19H18FN5O2
 1
1 IC50 = 7 nM
CP0176878
2-methoxy-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyridine-3-carboxamide
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C17H15F3N6O2
 1
1 IC50 = 7 nM
CP0176879
5-fluoro-2-methoxy-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyridine-3-carboxamide
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C17H14F4N6O2
 1
1 IC50 = 7 nM
CP0355864
N-[6-[4-(1-hydroxypropan-2-yl)-1,2,4-triazol-3-yl]pyridin-2-yl]-3-methoxy-1-methylpyrazole-4-carboxamide
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C16H19N7O3
 1
1 IC50 = 7 nM
CP0552416
4-methyl-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]-2,3-dihydro-1,4-benzoxazine-8-carboxamide
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C20H19F3N6O2
 1
1 IC50 = 7 nM
CP0354743
3-methoxy-1-(2-methoxyethyl)-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]pyrazole-4-carboxamide
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C18H23N7O3
 1
1 IC50 = 7.3 nM
CP0096219
BDBM50505948
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C18H16FN5O2
 1
1 IC50 = 8 nM
CP0188713
15-methylsulfonyl-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12(17),13,15,20,22-octaen-18-one
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C19H19N5O4S
 1
1 IC50 = 8 nM
CP0233898
(8R)-14-fluoro-8-methyl-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12(17),13,15,20,22-octaen-18-one
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C19H18FN5O2
 1
1 IC50 = 8 nM
CP0259270
15-morpholin-4-yl-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12(17),13,15,20,22-octaen-18-one
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C22H24N6O3
 2
1 IC50 = 8 nM
2 IC50 <= 100 nM
CP0326339
(8R)-15-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]-14-fluoro-8-methyl-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12(17),13,15,20,22-octaen-18-one
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C26H29FN8O2
 1
1 IC50 = 8 nM
CP0561695
3-methoxy-1-methyl-N-[6-[4-[(3S)-oxolan-3-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyrazole-4-carboxamide
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C17H19N7O3
 1
1 IC50 = 8 nM
CP0558673
3-methoxy-1-methyl-N-[6-[4-(1,1,1-trifluoropropan-2-yl)-1,2,4-triazol-3-yl]pyridin-2-yl]pyrazole-4-carboxamide
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C16H16F3N7O2
 1
1 IC50 = 9 nM
CP0326335
11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12,14,16,20,22-octaen-18-one
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C18H17N5O2
 1
1 IC50 = 11 nM
CP0384160
(9R)-9-methyl-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12,14,16,20,22-octaen-18-one
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C19H19N5O2
 2
1 IC50 = 13 nM
2 IC50 <= 100 nM
CP0188712
(8R)-8-methyl-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12,14,16,20,22-octaen-18-one
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C19H19N5O2
 1
1 IC50 = 14 nM
CP0125433
3-methoxy-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]-1-pyrimidin-5-ylpyrazole-4-carboxamide
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C19H19N9O2
 1
1 IC50 = 16 nM
CP0356982
BDBM50505947
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C18H16FN5O2
 1
1 IC50 = 17 nM
CP0540783
3-methoxy-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]-1-pyridin-2-ylpyrazole-4-carboxamide
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C20H20N8O2
 1
1 IC50 = 17 nM
CP0570802
4-methoxy-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyrimidine-5-carboxamide
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C16H14F3N7O2
 1
1 IC50 = 17 nM
CP0096218
N-[4-(6,7-dimethoxycinnolin-4-yl)oxyphenyl]-4-oxo-1-propan-2-ylquinoline-3-carboxamide
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C29H26N4O5
 1
1 IC50 = 18 nM
CP0561313
1-methyl-2-oxo-N-[6-[4-[(2S)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyridine-3-carboxamide
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C17H15F3N6O2
 1
1 IC50 = 18 nM
CP0356981
12-oxa-3,4,6,20,25-pentazatetracyclo[19.3.1.02,6.013,18]pentacosa-1(25),2,4,13,15,17,21,23-octaen-19-one
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C19H19N5O2
 2
1 IC50 = 20 nM
2 IC50 <= 100 nM
CP0517075
N-[6-[4-(3,3-difluorocyclobutyl)-1,2,4-triazol-3-yl]pyridin-2-yl]-3-methoxy-1-methylpyrazole-4-carboxamide
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C17H17F2N7O2
 1
1 IC50 = 20 nM
CP0163191
3-methoxy-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]-1-pyrazin-2-ylpyrazole-4-carboxamide
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C19H19N9O2
 1
1 IC50 = 21 nM
CP0343393
3-[3-[1-(methoxymethyl)pyrazol-4-yl]phenyl]-5-(4-propan-2-yl-1,2,4-triazol-3-yl)-1H-indazole
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C23H23N7O
 1
1 IC50 = 26.9 nM
CP0326337
15-(2-oxa-6-azaspiro[3.3]heptan-6-yl)-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12(17),13,15,20,22-octaen-18-one
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C23H24N6O3
 1
1 IC50 = 28 nM
CP0127753
1-methyl-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]pyrazole-3-carboxamide
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C15H17N7O
 1
1 IC50 = 29 nM
CP0748625
3-(3-(1-(1-ethoxyethyl)-1H-pyrazol-4-yl)phenyl)-5-(4-isopropyl-4H-1,2,4-triazol-3-yl)-1H-indazole
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C25H27N7O
 1
1 IC50 = 29.9 nM
CP0564282
3-methoxy-N-[6-[4-[(2R)-1-methoxypropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]-1-methylpyrazole-4-carboxamide
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C17H21N7O3
 1
1 IC50 = 31 nM
CP0176831
4-[2-(4-cyclopropylimidazol-1-yl)-4-[5-(4-propan-2-yl-1,2,4-triazol-3-yl)-1H-indazol-3-yl]phenyl]morpholine
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C28H30N8O
 1
1 IC50 = 31.8 nM
CP0562338
3-[3-(3-cyclopropyl-1,2,4-triazol-1-yl)phenyl]-5-(4-propan-2-yl-1,2,4-triazol-3-yl)-1H-indazole
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C23H22N8
 1
1 IC50 = 37 nM
CP0517074
N-[6-[4-[(2R)-1,1-difluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]-3-methoxy-1-methylpyrazole-4-carboxamide
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C16H17F2N7O2
 1
1 IC50 = 37 nM
CP0534062
3-methoxy-N-[6-[4-[(2S)-1-methoxypropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]-1-methylpyrazole-4-carboxamide
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C17H21N7O3
 1
1 IC50 = 44 nM
CP0471097
3-[3-(4-cyclopropylimidazol-1-yl)-5-methoxyphenyl]-5-(4-propan-2-yl-1,2,4-triazol-3-yl)-1H-indazole
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C25H25N7O
 1
1 IC50 = 48.6 nM
CP0558777
3-[3-(4-cyclopropylimidazol-1-yl)phenyl]-5-(4-cyclopropyl-1,2,4-triazol-3-yl)-1H-indazole
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C24H21N7
 1
1 IC50 = 50 nM
CP0271586
3-[3-[1-(oxan-4-yl)pyrazol-4-yl]phenyl]-5-(4-propan-2-yl-1,2,4-triazol-3-yl)-1H-indazole
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C26H27N7O
 1
1 IC50 = 50.1 nM
CP0487471
5-(4-cyclopentyl-1,2,4-triazol-3-yl)-3-[3-(4-cyclopropylimidazol-1-yl)phenyl]-1H-indazole
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C26H25N7
 1
1 IC50 = 54.1 nM
CP0181251
2-fluoro-4-methyl-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]benzamide
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C18H18FN5O
 1
1 IC50 = 55 nM
CP0419108
3-[3-(4-cyclopropylimidazol-1-yl)-4-methylphenyl]-5-(4-propan-2-yl-1,2,4-triazol-3-yl)-1H-indazole
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C25H25N7
 1
1 IC50 = 56.9 nM
CP0258310
3-[3-(1-methylpyrazol-4-yl)phenyl]-5-(4-propan-2-yl-1,2,4-triazol-3-yl)-1H-indazole
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C22H21N7
 1
1 IC50 = 63.6 nM
CP0228880
5-(4-cyclobutyl-1,2,4-triazol-3-yl)-3-[3-(4-cyclopropylimidazol-1-yl)phenyl]-1H-indazole
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C25H23N7
 1
1 IC50 = 70 nM
CP0188711
2-fluoro-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]benzamide
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C17H16FN5O
 2
1 IC50 = 76 nM
2 IC50 = 100 nM
CP0247995
N-[5-(cyclopropylamino)-7-(trifluoromethyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]pyridine-3-carboxamide
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C16H13F3N6O
 3
1 IC50 = 90 nM
2 IC50 = 93 nM
3 IC50 = 131 nM
CP0491476
2-methoxy-N-[6-(4-methyl-1,2,4-triazol-3-yl)pyridin-2-yl]benzamide
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C16H15N5O2
 1
1 IC50 = 92 nM
CP0565298
3-methoxy-1-methyl-N-[6-[4-[(2R)-1,1,1-trifluoropropan-2-yl]-1,2,4-triazol-3-yl]pyridin-2-yl]pyrazole-4-carboxamide
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C16H16F3N7O2
 1
1 IC50 = 94 nM
CP0197534
US11168095, Example 42
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C23H23N7O2
 1
1 IC50 <= 100 nM
CP0204700
US11168095, Example 18
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C19H19N5O2
 1
1 IC50 <= 100 nM
CP0416537
1-methyl-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]pyrazole-4-carboxamide
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C15H17N7O
 1
1 IC50 = 108 nM
CP0557069
3-methoxy-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]-1-pyridin-4-ylpyrazole-4-carboxamide
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C20H20N8O2
 1
1 IC50 = 134 nM
CP0326334
10-oxa-3,4,6,18,23-pentazatetracyclo[17.3.1.02,6.011,16]tricosa-1(23),2,4,11,13,15,19,21-octaen-17-one
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C17H15N5O2
 1
1 IC50 = 161 nM
CP0450705
(10S)-10-methyl-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12,14,16,20,22-octaen-18-one
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C19H19N5O2
 1
1 IC50 = 165 nM
CP0469369
(7R)-7-methyl-11-oxa-3,4,6,19,24-pentazatetracyclo[18.3.1.02,6.012,17]tetracosa-1(24),2,4,12,14,16,20,22-octaen-18-one
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C19H19N5O2
 1
1 IC50 = 350 nM
CP0559851
N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]benzamide
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C17H17N5O
 1
1 IC50 = 607 nM
CP0154571
5-(4-cyclopropylimidazol-1-yl)-2-fluoro-4-methyl-N-pyridin-2-ylbenzamide
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C19H17FN4O
 1
1 IC50 = 6000 nM
CP0339225
3-methoxy-1-methyl-N-[3-(4-propan-2-yl-1,2,4-triazol-3-yl)phenyl]pyrazole-4-carboxamide
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C17H20N6O2
 1
1 IC50 = 6164 nM
Clinical Information about the Protein
Target 1 ( Apoptosis signal-regulating kinase 1 (MAP3K5) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Diabetic nephropathy [ICD-11: GB61.Z]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 GS-4997 Phase 2
Diabetic nephropathy