General Information of the Protein
Protein ID
PT02105
Protein Name
Mitogen-activated protein kinase 7
Secondarily
Protein Name
Big MAP kinase 1
Extracellular signal-regulated kinase 5
Gene Name
MAPK7
Secondarily
Gene Name
BMK1
ERK5
PRKM7
Sequence
MAEPLKEEDGEDGSAEPPGPVKAEPAHTAASVAAKNLALLKARSFDVTFDVGDEYEIIETIGNGAYGVVSSARRRLTGQQVAIKKIPNAFDVVTNAKRTLRELKILKHFKHDNIIAIKDILRPTVPYGEFKSVYVVLDLMESDLHQIIHSSQPLTLEHVRYFLYQLLRGLKYMHSAQVIHRDLKPSNLLVNENCELKIGDFGMARGLCTSPAEHQYFMTEYVATRWYRAPELMLSLHEYTQAIDLWSVGCIFGEMLARRQLFPGKNYVHQLQLIMMVLGTPSPAVIQAVGAERVRAYIQSLPPRQPVPWETVYPGADRQALSLLGRMLRFEPSARISAAAALRHPFLAKYHDPDDEPDCAPPFDFAFDREALTRERIKEAIVAEIEDFHARREGIRQQIRFQPSLQPVASEPGCPDVEMPSPWAPSGDCAMESPPPAPPPCPGPAPDTIDLTLQPPPPVSEPAPPKKDGAISDNTKAALKAALLKSLRSRLRDGPSAPLEAPEPRKPVTAQERQREREEKRRRRQERAKEREKRRQERERKERGAGASGGPSTDPLAGLVLSDNDRSLLERWTRMARPAAPALTSVPAPAPAPTPTPTPVQPTSPPPGPVAQPTGPQPQSAGSTSGPVPQPACPPPGPAPHPTGPPGPIPVPAPPQIATSTSLLAAQSLVPPPGLPGSSTPGVLPYFPPGLPPPDAGGAPQSSMSESPDVNLVTQQLSKSQVEDPLPPVFSGTPKGSGAGYGVGFDLEEFLNQSFDMGVADGPQDGQADSASLSASLLADWLEGHGMNPADIESLQREIQMDSPMLLADLPDLQDP
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CMGC protein kinase group
>
CMGC protein kinase MAPK family
>
CMGC protein kinase ERK5
Function
Plays a role in various cellular processes such as proliferation, differentiation and cell survival. The upstream activator of MAPK7 is the MAPK kinase MAP2K5. Upon activation, it translocates to the nucleus and phosphorylates various downstream targets including MEF2C. EGF activates MAPK7 through a Ras-independent and MAP2K5-dependent pathway. May have a role in muscle cell differentiation. May be important for endothelial function and maintenance of blood vessel integrity. MAP2K5 and MAPK7 interact specifically with one another and not with MEK1/ERK1 or MEK2/ERK2 pathways. Phosphorylates SGK1 at Ser-78 and this is required for growth factor-induced cell cycle progression. Involved in the regulation of p53/TP53 by disrupting the PML-MDM2 interaction.
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Uniprot ID
Primary ID:
Q13164

Secondarily ID:
Q16634
Q59F50
Q6QLU7
Q7L4P4
Q969G1
Q96G51
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Ensembl ID
ENSG00000166484
HGNC ID
HGNC:6880
Subcellular Location
Cytoplasm
Nucleus
Nucleus
PML body
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: CL000017 , HeLa
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0436072
 Compound Info 
2-[2-ethoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5-methyl-11-methylsulfonylpyrimido[4,5-b][1,4]benzodiazepin-6-one
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C32H40N8O5S
  1
1
IC50 = 8 nM
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CP0579131
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[2-[(4-methylpiperazin-1-yl)methyl]pyrimidin-5-yl]-1H-pyrrole-2-carboxamide
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C22H21Cl2FN6O2
  1
1
IC50 = 20 nM
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CP0579555
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[6-[(1-methylpiperidin-4-yl)methyl]pyridin-3-yl]-1H-pyrrole-2-carboxamide
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C24H23Cl2FN4O2
  1
1
IC50 = 31 nM
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CP0568064
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[2-[(1-methylpiperidin-4-yl)amino]pyrimidin-5-yl]-1H-pyrrole-2-carboxamide
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C22H21Cl2FN6O2
  1
1
IC50 = 43 nM
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CP0577393
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[6-(1-methylpiperidin-4-yl)oxypyridin-3-yl]-1H-pyrrole-2-carboxamide
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C23H21Cl2FN4O3
  1
1
IC50 = 58 nM
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CP0577392
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[2-(piperazin-1-ylmethyl)pyrimidin-5-yl]-1H-pyrrole-2-carboxamide
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C21H19Cl2FN6O2
  1
1
IC50 = 60 nM
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CP0377465
 Compound Info 
11-ethyl-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-5-methyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C26H31N7O2
  2
1
IC50 = 66 nM
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2
IC50 = 200 nM
 Bioactivity Info 
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CP0551933
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[6-[(4-methylpiperazin-1-yl)methyl]pyridin-3-yl]-1H-pyrrole-2-carboxamide
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C23H22Cl2FN5O2
  1
1
IC50 = 70 nM
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CP0491701
 Compound Info 
11-cyclobutyl-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-5-methylpyrimido[4,5-b][1,4]benzodiazepin-6-one
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C28H33N7O2
  1
1
IC50 = 79 nM
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CP0051871
 Compound Info 
2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C25H29N7O2
  2
1
IC50 = 87 nM
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2
IC50 = 190 nM
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CP0380419
 Compound Info 
11-isopropyl-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-5-methyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C27H33N7O2
  2
1
IC50 = 98 nM
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2
IC50 = 230 nM
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CP0404446
 Compound Info 
2-((2-methoxy-4-(4-(pyrrolidin-1-yl)piperidine-1-carbonyl)phenyl)amino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C30H35N7O3
  1
1
IC50 = 130 nM
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CP0570478
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-(1-methylpyrazol-4-yl)-1H-pyrrole-2-carboxamide
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C16H11Cl2FN4O2
  1
1
IC50 = 141 nM
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CP0473882
 Compound Info 
11-cyclopentyl-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-5-methyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C29H35N7O2
  2
1
IC50 = 146 nM
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2
IC50 = 200 nM
 Bioactivity Info 
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CP0454393
 Compound Info 
2-((2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C30H38N8O2
  1
1
IC50 = 200 nM
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CP0535040
 Compound Info 
11-butan-2-yl-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-5-methylpyrimido[4,5-b][1,4]benzodiazepin-6-one
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C28H35N7O2
  1
1
IC50 = 222 nM
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CP0404445
 Compound Info 
2-((2-methoxy-4-(piperazin-1-yl)phenyl)amino)-5,11-dimethyl-5H-benzo[e]-pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C24H27N7O2
  1
1
IC50 = 230 nM
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CP0074960
 Compound Info 
2-((2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl)amino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C26H30N6O3
  2
1
IC50 = 240 nM
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2
IC50 = 300 nM
 Bioactivity Info 
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CP0365412
 Compound Info 
2-((4-(4-hydroxypiperidin-1-yl)-2-methoxyphenyl)amino-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C25H28N6O3
  1
1
IC50 = 240 nM
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CP0404447
 Compound Info 
4-((5,11-dimethyl-6-oxo-6,11-dihydro-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-2-yl)amino)-N-(2-(dimethylamino)ethyl)-3-methoxybenzamide
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C25H29N7O3
  1
1
IC50 = 240 nM
 Bioactivity Info 
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CP0404448
 Compound Info 
2-((2-methoxy-4-(1-methylpiperidin-4-yl)phenyl)amino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C26H30N6O2
  1
1
IC50 = 260 nM
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CP0454361
 Compound Info 
2-((2-methoxy-4-morpholinophenyl)amino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C24H26N6O3
  1
1
IC50 = 260 nM
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CP0363540
 Compound Info 
N-[4-[(5,11-dimethyl-6-oxopyrimido[4,5-b][1,4]benzodiazepin-2-yl)amino]-3-methoxyphenyl]methanesulfonamide
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C21H22N6O4S
  1
1
IC50 = 276 nM
 Bioactivity Info 
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CP0404450
 Compound Info 
5,11-dimethyl-2-((2-methyl-4-(4-methylpiperazin-1-yl)phenyl)amino)-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C25H29N7O
  1
1
IC50 = 280 nM
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CP0395994
 Compound Info 
4-((5,11-dimethyl-6-oxo-6,11-dihydro-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-2-yl)amino)benzenesulfonamide
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C19H18N6O3S
  1
1
IC50 = 310 nM
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CP0357714
 Compound Info 
4-((5,11-dimethyl-6-oxo-6,11-dihydro-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-2-yl)amino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
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C27H31N7O3
  1
1
IC50 = 320 nM
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CP0473027
 Compound Info 
4-[(5-ethyl-11-methyl-6-oxopyrimido[4,5-b][1,4]benzodiazepin-2-yl)amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
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C28H33N7O3
  1
1
IC50 = 482 nM
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CP0570111
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[1-(piperidin-4-ylmethyl)pyrazol-4-yl]-1H-pyrrole-2-carboxamide
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C21H20Cl2FN5O2
  1
1
IC50 = 671 nM
 Bioactivity Info 
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CP0570110
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-(1-piperidin-4-ylpyrazol-4-yl)-1H-pyrrole-2-carboxamide
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C20H18Cl2FN5O2
  1
1
IC50 = 787 nM
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CP0437474
 Compound Info 
9-chloro-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C25H28ClN7O2
  2
1
IC50 = 1138 nM
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2
IC50 = 11380 nM
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CP0085569
 Compound Info 
2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)-11-methyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C24H27N7O2
  1
1
IC50 = 1200 nM
 Bioactivity Info 
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CP0266619
 Compound Info 
5-ethyl-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-11-methylpyrimido[4,5-b][1,4]benzodiazepin-6-one
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C26H31N7O2
  1
1
IC50 = 1200 nM
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CP0465764
 Compound Info 
8-chloro-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C25H28ClN7O2
  1
1
IC50 = 1240 nM
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CP0454394
 Compound Info 
9-fluoro-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C25H28FN7O2
  1
1
IC50 = 1320 nM
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CP0380420
 Compound Info 
2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-5,8,11-trimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C26H31N7O2
  1
1
IC50 = 3100 nM
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CP0437475
 Compound Info 
2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-11-methyl-5-(2,2,2-trifluoroethyl)pyrimido[4,5-b][1,4]benzodiazepin-6-one
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C26H28F3N7O2
  1
1
IC50 = 3350 nM
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CP0473026
 Compound Info 
2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-4,5,11-trimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one
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C26H31N7O2
  1
1
IC50 > 10000 nM
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Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Cell Line ID: CL000307 , SN12C
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0074960
 Compound Info 
2-((2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl)amino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C26H30N6O3
  2
1 EC50 < 5000 nM
2 Kd = 80 nM
CP0551933
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[6-[(4-methylpiperazin-1-yl)methyl]pyridin-3-yl]-1H-pyrrole-2-carboxamide
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C23H22Cl2FN5O2
  1
1 IC50 = 5 nM
CP0579555
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[6-[(1-methylpiperidin-4-yl)methyl]pyridin-3-yl]-1H-pyrrole-2-carboxamide
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C24H23Cl2FN4O2
  1
1 IC50 = 6 nM
CP0570111
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[1-(piperidin-4-ylmethyl)pyrazol-4-yl]-1H-pyrrole-2-carboxamide
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C21H20Cl2FN5O2
  1
1 IC50 = 7 nM
CP0579131
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[2-[(4-methylpiperazin-1-yl)methyl]pyrimidin-5-yl]-1H-pyrrole-2-carboxamide
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C22H21Cl2FN6O2
  1
1 IC50 = 7 nM
CP0436072
 Compound Info 
2-[2-ethoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5-methyl-11-methylsulfonylpyrimido[4,5-b][1,4]benzodiazepin-6-one
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C32H40N8O5S
  1
1 IC50 = 8 nM
CP0577392
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[2-(piperazin-1-ylmethyl)pyrimidin-5-yl]-1H-pyrrole-2-carboxamide
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C21H19Cl2FN6O2
  1
1 IC50 = 8 nM
CP0568064
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[2-[(1-methylpiperidin-4-yl)amino]pyrimidin-5-yl]-1H-pyrrole-2-carboxamide
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C22H21Cl2FN6O2
  1
1 IC50 = 14 nM
CP0577393
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-[6-(1-methylpiperidin-4-yl)oxypyridin-3-yl]-1H-pyrrole-2-carboxamide
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C23H21Cl2FN4O3
  1
1 IC50 = 14 nM
CP0570110
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-(1-piperidin-4-ylpyrazol-4-yl)-1H-pyrrole-2-carboxamide
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C20H18Cl2FN5O2
  1
1 IC50 = 19 nM
CP0024313
 Compound Info 
[2-amino-4-(trifluoromethoxy)phenyl]-[4-[7-(4-methylpiperazin-1-yl)pyrido[3,2-d]pyrimidin-4-yl]piperidin-1-yl]methanone
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C25H28F3N7O2
  1
1 IC50 = 35 nM
CP0570478
 Compound Info 
4-(3,6-dichloro-2-fluorobenzoyl)-N-(1-methylpyrazol-4-yl)-1H-pyrrole-2-carboxamide
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C16H11Cl2FN4O2
  1
1 IC50 = 79 nM
CP0260249
 Compound Info 
11-cyclopentyl-2-[2-ethoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5-methylpyrimido[4,5-b][1,4]benzodiazepin-6-one
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C36H46N8O3
  1
1 IC50 = 162 nM
CP0051871
 Compound Info 
2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C25H29N7O2
  1
1 Kd = 19 nM
CP0365412
 Compound Info 
2-((4-(4-hydroxypiperidin-1-yl)-2-methoxyphenyl)amino-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C25H28N6O3
  1
1 Kd = 57 nM
CP0085569
 Compound Info 
2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)-11-methyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
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C24H27N7O2
  2
1 Kd = 670 nM
2 Kd > 670 nM
Clinical Information about the Protein
Target 1 ( Extracellular signal-regulated kinase 5 (ERK5) )
Target Type Patented-recorded Target