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Target
Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha
Ligand
BDBM6309
Substrate
n/a
Meas. Tech.
ChEMBL_2299890
IC50
208±n/a nM
Citation
 Willems, HMG; Edwards, S; Boffey, HK; Chawner, SJ; Green, C; Romero, T; Winpenny, D; Skidmore, J; Clarke, JH; Andrews, SP Identification of ARUK2002821 as an isoform-selective PI5P4K? inhibitor. RSC Med Chem 14:934-946 (2023) [PubMed] 
Target
Name:
Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha
Synonyms:
1-phosphatidylinositol 5-phosphate 4-kinase 2-alpha | 2.7.1.149 | Diphosphoinositide kinase 2-alpha | PI(5)P 4-kinase type II alpha | PI42A_HUMAN | PI5P4KA | PIP4K2A | PIP4KII-alpha | PIP5K2 | PIP5K2A | PIP5KIII | Phosphatidylinositol 5-phosphate 4-kinase type II alpha | Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha | Phosphatidylinositol-5-phosphate 4-kinase type-2 alpha | PtdIns(4)P-5-kinase B isoform | PtdIns(4)P-5-kinase C isoform | PtdIns(5)P-4-kinase isoform 2-alpha
Type:
PROTEIN
Mol. Mass.:
46228.59
Organism:
Homo sapiens
Description:
ChEMBL_104274
Residue:
406
Sequence:
MATPGNLGSSVLASKTKTKKKHFVAQKVKLFRASDPLLSVLMWGVNHSINELSHVQIPVMLMPDDFKAYSKIKVDNHLFNKENMPSHFKFKEYCPMVFRNLRERFGIDDQDFQNSLTRSAPLPNDSQARSGARFHTSYDKRYIIKTITSEDVAEMHNILKKYHQYIVECHGITLLPQFLGMYRLNVDGVEIYVIVTRNVFSHRLSVYRKYDLKGSTVAREASDKEKAKELPTLKDNDFINEGQKIYIDDNNKKVFLEKLKKDVEFLAQLKLMDYSLLVGIHDVERAEQEEVECEENDGEEEGESDGTHPVGTPPDSPGNTLNSSPPLAPGEFDPNIDVYGIKCHENSPRKEVYFMAIIDILTHYDAKKKAAHAAKTVKHGAGAEISTVNPEQYSKRFLDFIGHILT
  
Inhibitor
Name:
BDBM6309
Synonyms:
6-Acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one Hydrochloride | 8-cyclopentyl-6-acetyl-5-methyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H,8H-pyrido[2,3-d]pyrimidin-7-one | Ibrance | PD 0332991 | Palbociclib | Pyrido-[2,3-d]-pyrimidin-7-one 43 | US10189849, PD0332991 | US10464927, Compound Palbociclib | US10626107, Example Palbociclib | US10696682, Compound PD0332991 | US10927120, PD0332991 | US9464092, PD0332991 | US9957276, PD0332991
Type:
Small organic molecule
Emp. Form.:
C24H29N7O2
Mol. Mass.:
447.5328
SMILES:
CC(=O)c1c(C)c2cnc(Nc3ccc(cn3)N3CCNCC3)nc2n(C2CCCC2)c1=O
Structure:
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