Target
Mitogen-activated protein kinase 7
Ligand
BDBM50516388
Substrate
n/a
Meas. Tech.
ChEMBL_1864570 (CHEMBL4365545)
IC50
600±n/a nM
Citation
 Myers, SMMiller, DCMolyneux, LArasta, MBawn, RHBlackburn, TJCook, SJEdwards, NEndicott, JAGolding, BTGriffin, RJHammonds, THardcastle, IRHarnor, SJHeptinstall, ABLochhead, PAMartin, MPMartin, NCNewell, DROwen, PJPang, LCReuillon, TRigoreau, LJMThomas, HDTucker, JAWang, LZWong, ACNoble, MEMWedge, SRCano, C Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38? and BRD4. Eur J Med Chem 178:530-543 (2019) [PubMed]  Article 
Target
Name:
Mitogen-activated protein kinase 7
Synonyms:
BMK1 | Big MAP kinase 1 | ERK5 | Extracellular signal-regulated kinase 5 (ERK5) | MAPK7 | MK07_HUMAN | PRKM7
Type:
Protein
Mol. Mass.:
88377.36
Organism:
Homo sapiens (Human)
Description:
Q13164
Residue:
816
Sequence:
MAEPLKEEDGEDGSAEPPGPVKAEPAHTAASVAAKNLALLKARSFDVTFDVGDEYEIIETIGNGAYGVVSSARRRLTGQQVAIKKIPNAFDVVTNAKRTLRELKILKHFKHDNIIAIKDILRPTVPYGEFKSVYVVLDLMESDLHQIIHSSQPLTLEHVRYFLYQLLRGLKYMHSAQVIHRDLKPSNLLVNENCELKIGDFGMARGLCTSPAEHQYFMTEYVATRWYRAPELMLSLHEYTQAIDLWSVGCIFGEMLARRQLFPGKNYVHQLQLIMMVLGTPSPAVIQAVGAERVRAYIQSLPPRQPVPWETVYPGADRQALSLLGRMLRFEPSARISAAAALRHPFLAKYHDPDDEPDCAPPFDFAFDREALTRERIKEAIVAEIEDFHARREGIRQQIRFQPSLQPVASEPGCPDVEMPSPWAPSGDCAMESPPPAPPPCPGPAPDTIDLTLQPPPPVSEPAPPKKDGAISDNTKAALKAALLKSLRSRLRDGPSAPLEAPEPRKPVTAQERQREREEKRRRRQERAKEREKRRQERERKERGAGASGGPSTDPLAGLVLSDNDRSLLERWTRMARPAAPALTSVPAPAPAPTPTPTPVQPTSPPPGPVAQPTGPQPQSAGSTSGPVPQPACPPPGPAPHPTGPPGPIPVPAPPQIATSTSLLAAQSLVPPPGLPGSSTPGVLPYFPPGLPPPDAGGAPQSSMSESPDVNLVTQQLSKSQVEDPLPPVFSGTPKGSGAGYGVGFDLEEFLNQSFDMGVADGPQDGQADSASLSASLLADWLEGHGMNPADIESLQREIQMDSPMLLADLPDLQDP
  
Inhibitor
Name:
BDBM50516388
Synonyms:
CHEMBL4453232
Type:
Small organic molecule
Emp. Form.:
C17H11ClFN3O2
Mol. Mass.:
343.74
SMILES:
Fc1cccc(Cl)c1C(=O)c1c[nH]c(c1)C(=O)Nc1cccnc1
Structure:
Search PDB for entries with ligand similarity: