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Target
Mitogen-activated protein kinase 11
Ligand
BDBM50327009
Substrate
n/a
Meas. Tech.
ChEMBL_972021 (CHEMBL2405972)
IC50
62±n/a nM
Citation
Wrobleski, ST; Lin, S; Dhar, TG; Dyckman, AJ; Li, T; Pitt, S; Zhang, R; Fan, Y; Doweyko, AM; Tokarski, JS; Kish, KF; Kiefer, SE; Sack, JS; Newitt, JA; Witmer, MR; McKinnon, M; Barrish, JC; Dodd, JH; Schieven, GL; Leftheris, K The identification of novel p38? isoform selective kinase inhibitors having an unprecedented p38? binding mode. Bioorg Med Chem Lett 23:4120-6 (2013) [PubMed] Article
More Info.:
Target
Name:
Mitogen-activated protein kinase 11
Synonyms:
MAP kinase p38 | MAPK11 | MK11_HUMAN | Mitogen-activated protein kinase 11 | Mitogen-activated protein kinase p38 beta | PRKM11 | SAPK2 | SAPK2B | Stress-activated protein kinase 2 | p38 MAP kinase alpha/beta | p38-2 | p38-beta | p38b
Type:
Enzyme Catalytic Domain
Mol. Mass.:
41351.73
Organism:
Homo sapiens (Human)
Description:
gi_20128774
Residue:
364
Sequence:
MSGPRAGFYRQELNKTVWEVPQRLQGLRPVGSGAYGSVCSAYDARLRQKVAVKKLSRPFQSLIHARRTYRELRLLKHLKHENVIGLLDVFTPATSIEDFSEVYLVTTLMGADLNNIVKCQALSDEHVQFLVYQLLRGLKYIHSAGIIHRDLKPSNVAVNEDCELRILDFGLARQADEEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLQGKALFPGSDYIDQLKRIMEVVGTPSPEVLAKISSEHARTYIQSLPPMPQKDLSSIFRGANPLAIDLLGRMLVLDSDQRVSAAEALAHAYFSQYHDPEDEPEAEPYDESVEAKERTLEEWKELTYQEVLSFKPPEPPKPPGSLEIEQ
Inhibitor
Name:
BDBM50327009
Synonyms:
4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide | 4-{[5-(cyclopropylcarbamoyl)-2-methylphenyl]amino}-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide | CHEMBL1230065
Type:
Small organic molecule
Emp. Form.:
C22H26N6O2
Mol. Mass.:
406.4808
SMILES:
CCCNC(=O)c1cn2ncnc(Nc3cc(ccc3C)C(=O)NC3CC3)c2c1C