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Target
Serine/threonine-protein kinase pim-1/pim-2/pim-3
Ligand
BDBM192539
Substrate
n/a
Meas. Tech.
ChEMBL_1622455 (CHEMBL3864807)
IC50
403±n/a nM
Citation
 Wurz, RP; Sastri, C; D'Amico, DC; Herberich, B; Jackson, CLM; Pettus, LH; Tasker, AS; Wu, B; Guerrero, N; Lipford, JR; Winston, JT; Yang, Y; Wang, P; Nguyen, Y; Andrews, KL; Huang, X; Lee, MR; Mohr, C; Zhang, JD; Reid, DL; Xu, Y; Zhou, Y; Wang, HL Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors. Bioorg Med Chem Lett 26:5580-5590 (2016) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase pim-1/pim-2/pim-3
Synonyms:
Serine/threonine-protein kinase PIM
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 2135988
Components:
This complex has 3 components.
Component 1
Name:
Serine/threonine-protein kinase pim-1
Synonyms:
PIM-1 Kinase | PIM1 | PIM1_HUMAN | Proto-oncogene serine/threonine-protein kinase Pim-1 | Serine/threonine-protein kinase (PIM1) | Serine/threonine-protein kinase PIM | Serine/threonine-protein kinase PIM1 | Serine/threonine-protein kinase pim-1 (PIM1)
Type:
Protein
Mol. Mass.:
35681.82
Organism:
Homo sapiens (Human)
Description:
P11309
Residue:
313
Sequence:
MLLSKINSLAHLRAAPCNDLHATKLAPGKEKEPLESQYQVGPLLGSGGFGSVYSGIRVSDNLPVAIKHVEKDRISDWGELPNGTRVPMEVVLLKKVSSGFSGVIRLLDWFERPDSFVLILERPEPVQDLFDFITERGALQEELARSFFWQVLEAVRHCHNCGVLHRDIKDENILIDLNRGELKLIDFGSGALLKDTVYTDFDGTRVYSPPEWIRYHRYHGRSAAVWSLGILLYDMVCGDIPFEHDEEIIRGQVFFRQRVSSECQHLIRWCLALRPSDRPTFEEIQNHPWMQDVLLPQETAEIHLHSLSPGPSK
  
Component 2
Name:
Serine/threonine-protein kinase pim-2
Synonyms:
PIM2 | PIM2_HUMAN | Pim-2h | Serine/threonine-protein kinase (PIM2) | Serine/threonine-protein kinase PIM | Serine/threonine-protein kinase pim-2 (PIM2)
Type:
Serine/threonine-protein kinase
Mol. Mass.:
34185.93
Organism:
Homo sapiens (Human)
Description:
Q9P1W9
Residue:
311
Sequence:
MLTKPLQGPPAPPGTPTPPPGGKDREAFEAEYRLGPLLGKGGFGTVFAGHRLTDRLQVAIKVIPRNRVLGWSPLSDSVTCPLEVALLWKVGAGGGHPGVIRLLDWFETQEGFMLVLERPLPAQDLFDYITEKGPLGEGPSRCFFGQVVAAIQHCHSRGVVHRDIKDENILIDLRRGCAKLIDFGSGALLHDEPYTDFDGTRVYSPPEWISRHQYHALPATVWSLGILLYDMVCGDIPFERDQEILEAELHFPAHVSPDCCALIRRCLAPKPSSRPSLEEILLDPWMQTPAEDVPLNPSKGGPAPLAWSLLP
  
Component 3
Name:
Serine/threonine-protein kinase pim-3
Synonyms:
PIM3 | PIM3_HUMAN | Serine/threonine-protein kinase pim-3 (PIM3)
Type:
Protein
Mol. Mass.:
35888.19
Organism:
Homo sapiens (Human)
Description:
Q86V86
Residue:
326
Sequence:
MLLSKFGSLAHLCGPGGVDHLPVKILQPAKADKESFEKAYQVGAVLGSGGFGTVYAGSRIADGLPVAVKHVVKERVTEWGSLGGATVPLEVVLLRKVGAAGGARGVIRLLDWFERPDGFLLVLERPEPAQDLFDFITERGALDEPLARRFFAQVLAAVRHCHSCGVVHRDIKDENLLVDLRSGELKLIDFGSGALLKDTVYTDFDGTRVYSPPEWIRYHRYHGRSATVWSLGVLLYDMVCGDIPFEQDEEILRGRLLFRRRVSPECQQLIRWCLSLRPSERPSLDQIAAHPWMLGADGGVPESCDLRLCTLDPDDVASTTSSSESL
  
Inhibitor
Name:
BDBM192539
Synonyms:
US9187486, 1
Type:
Small organic molecule
Emp. Form.:
C22H21F2N7
Mol. Mass.:
421.4458
SMILES:
N[C@H]1CCCN(C1)c1ccncc1Nc1ncc2ccc(nn12)-c1c(F)cccc1F |r|
Structure:
Search PDB for entries with ligand similarity: