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Target
Mitogen-activated protein kinase 11/12/13/14
Ligand
BDBM50122919
Substrate
n/a
Meas. Tech.
ChEMBL_212759 (CHEMBL818992)
IC50
400±n/a nM
Citation
Colletti, SL; Frie, JL; Dixon, EC; Singh, SB; Choi, BK; Scapin, G; Fitzgerald, CE; Kumar, S; Nichols, EA; O'Keefe, SJ; O'Neill, EA; Porter, G; Samuel, K; Schmatz, DM; Schwartz, CD; Shoop, WL; Thompson, CM; Thompson, JE; Wang, R; Woods, A; Zaller, DM; Doherty, JB Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones. J Med Chem 46:349-52 (2003) [PubMed] Article
More Info.:
Target
Name:
Mitogen-activated protein kinase 11/12/13/14
Synonyms:
MAP kinase p38
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 1935922
Components:
This complex has 4 components.
Component 1
Name:
Mitogen-activated protein kinase 13
Synonyms:
MAP kinase p38 delta | MAPK13 | MK13_HUMAN | Mitogen-activated protein kinase 13 | Mitogen-activated protein kinase 13 (MAPK13) | Mitogen-activated protein kinase p38 | Mitogen-activated protein kinase p38 delta | PRKM13 | SAPK4 | Stress-activated protein kinase 4 | p38 delta/gamma
Type:
Enzyme
Mol. Mass.:
42097.16
Organism:
Homo sapiens (Human)
Description:
O15264
Residue:
365
Sequence:
MSLIRKKGFYKQDVNKTAWELPKTYVSPTHVGSGAYGSVCSAIDKRSGEKVAIKKLSRPFQSEIFAKRAYRELLLLKHMQHENVIGLLDVFTPASSLRNFYDFYLVMPFMQTDLQKIMGMEFSEEKIQYLVYQMLKGLKYIHSAGVVHRDLKPGNLAVNEDCELKILDFGLARHADAEMTGYVVTRWYRAPEVILSWMHYNQTVDIWSVGCIMAEMLTGKTLFKGKDYLDQLTQILKVTGVPGTEFVQKLNDKAAKSYIQSLPQTPRKDFTQLFPRASPQAADLLEKMLELDVDKRLTAAQALTHPFFEPFRDPEEETEAQQPFDDSLEHEKLTVDEWKQHIYKEIVNFSPIARKDSRRRSGMKL
Component 2
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
Component 3
Name:
Mitogen-activated protein kinase 14
Synonyms:
CSAID-binding protein | CSBP | CSBP1 | CSBP2 | CSPB1 | Cytokine suppressive anti-inflammatory drug-binding protein | MAP kinase 14 | MAP kinase MXI2 | MAP kinase p38 alpha | MAPK 14 | MAPK14 | MAX-interacting protein 2 | MK14_HUMAN | MXI2 | Mitogen-activated protein kinase p38 alpha | SAPK2A | Stress-activated protein kinase 2a | p38 MAP kinase alpha/beta
Type:
Serine/threonine-protein kinase
Mol. Mass.:
41286.76
Organism:
Homo sapiens (Human)
Description:
Q16539
Residue:
360
Sequence:
MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQSIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQKLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVGTPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAAQALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES
Component 4
Name:
Mitogen-activated protein kinase 12
Synonyms:
ERK6 | MAP kinase p38 gamma | MAPK12 | MK12_HUMAN | Mitogen-activated protein kinase 12 (MAPK12 p38 gamma) | Mitogen-activated protein kinase 12 (p38 gamma) | Mitogen-activated protein kinase 12 Gamma | Mitogen-activated protein kinase p38 gamma (p38 MAPKγ) | SAPK3 | p38 delta/gamma
Type:
Protein
Mol. Mass.:
41938.69
Organism:
Homo sapiens (Human)
Description:
P53778
Residue:
367
Sequence:
MSSPPPARSGFYRQEVTKTAWEVRAVYRDLQPVGSGAYGAVCSAVDGRTGAKVAIKKLYRPFQSELFAKRAYRELRLLKHMRHENVIGLLDVFTPDETLDDFTDFYLVMPFMGTDLGKLMKHEKLGEDRIQFLVYQMLKGLRYIHAAGIIHRDLKPGNLAVNEDCELKILDFGLARQADSEMTGYVVTRWYRAPEVILNWMRYTQTVDIWSVGCIMAEMITGKTLFKGSDHLDQLKEIMKVTGTPPAEFVQRLQSDEAKNYMKGLPELEKKDFASILTNASPLAVNLLEKMLVLDAEQRVTAGEALAHPYFESLHDTEDEPQVQKYDDSFDDVDRTLDEWKRVTYKEVLSFKPPRQLGARVSKETPL
Inhibitor
Name:
BDBM50122919
Synonyms:
6-[2-(2-Chloro-4-fluoro-phenyl)-imidazo[1,2-a]pyridin-3-yl]-2-(2-chloro-phenyl)-4,5-dihydro-2H-pyridazin-3-one | CHEMBL118917
Type:
Small organic molecule
Emp. Form.:
C23H15Cl2FN4O
Mol. Mass.:
453.296
SMILES:
Fc1ccc(-c2nc3ccccn3c2C2=NN(C(=O)CC2)c2ccccc2Cl)c(Cl)c1 |t:16|