Target
Serine/threonine-protein kinase pim-1
Ligand
BDBM377249
Substrate
n/a
Meas. Tech.
Pim Enzyme Assay
IC50
<100±n/a nM
Citation
 Xue, CLi, YFeng, HZhang, K Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors US Patent  US10828290 Publication Date 11/10/2020 
Target
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
  
Inhibitor
Name:
BDBM377249
Synonyms:
US10265307, Example 72-2 | US10517858, Example 72 (Diastereoisomer 2) | US10828290, Example 72 (Diastereoisomer 2)
Type:
Small organic molecule
Emp. Form.:
C29H29F6N5O3
Mol. Mass.:
609.5627
SMILES:
CC(C)(O)c1cc(F)c(c(F)c1)-c1nc(ccc1F)C(=O)Nc1cnc2[C@H](O)CCc2c1N1C[C@@H](N)C[C@H](C1)C(F)(F)F |r,wU:34.38,37.43,wD:26.28,(7.85,-2.21,;7.85,-3.75,;7.85,-5.29,;9.19,-2.98,;6.52,-2.98,;6.52,-1.44,;5.19,-.67,;5.19,.87,;3.85,-1.44,;3.85,-2.98,;2.52,-3.75,;5.19,-3.75,;2.52,-.67,;1.18,-1.44,;-.15,-.67,;-.15,.87,;1.18,1.64,;2.52,.87,;3.85,1.64,;-1.48,-1.44,;-1.48,-2.98,;-2.82,-.67,;-4.15,-1.44,;-4.15,-2.98,;-5.48,-3.75,;-6.82,-2.98,;-8.28,-3.45,;-8.68,-4.94,;-9.19,-2.21,;-8.28,-.96,;-6.82,-1.44,;-5.48,-.67,;-5.48,.87,;-6.82,1.64,;-6.82,3.18,;-8.15,3.95,;-5.48,3.95,;-4.15,3.18,;-4.15,1.64,;-2.82,3.95,;-1.48,4.72,;-2.05,2.62,;-3.59,5.29,)|
Structure:
Search PDB for entries with ligand similarity: