Target
1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1
Ligand
BDBM107352
Substrate
n/a
Meas. Tech.
ITK Target Modulation PLC-gamma Assay
Temperature
310.15±n/a K
IC50
<1000±n/a nM
Comments
extracted
Citation
 Jacobsen, EJBlinn, JRSpringer, JRHockerman, SL Heterocyclic ITK inhibitors for treating inflammation and cancer US Patent  US9695200 Publication Date 7/4/2017 
Target
Name:
1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1
Synonyms:
PLC1 | PLCG1 | PLCG1_HUMAN | Phospholipase C-gamma-1
Type:
PROTEIN
Mol. Mass.:
148518.78
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1435182
Residue:
1290
Sequence:
MAGAASPCANGCGPGAPSDAEVLHLCRSLEVGTVMTLFYSKKSQRPERKTFQVKLETRQITWSRGADKIEGAIDIREIKEIRPGKTSRDFDRYQEDPAFRPDQSHCFVILYGMEFRLKTLSLQATSEDEVNMWIKGLTWLMEDTLQAPTPLQIERWLRKQFYSVDRNREDRISAKDLKNMLSQVNYRVPNMRFLRERLTDLEQRSGDITYGQFAQLYRSLMYSAQKTMDLPFLEASTLRAGERPELCRVSLPEFQQFLLDYQGELWAVDRLQVQEFMLSFLRDPLREIEEPYFFLDEFVTFLFSKENSVWNSQLDAVCPDTMNNPLSHYWISSSHNTYLTGDQFSSESSLEAYARCLRMGCRCIELDCWDGPDGMPVIYHGHTLTTKIKFSDVLHTIKEHAFVASEYPVILSIEDHCSIAQQRNMAQYFKKVLGDTLLTKPVEISADGLPSPNQLKRKILIKHKKLAEGSAYEEVPTSMMYSENDISNSIKNGILYLEDPVNHEWYPHYFVLTSSKIYYSEETSSDQGNEDEEEPKEVSSSTELHSNEKWFHGKLGAGRDGRHIAERLLTEYCIETGAPDGSFLVRESETFVGDYTLSFWRNGKVQHCRIHSRQDAGTPKFFLTDNLVFDSLYDLITHYQQVPLRCNEFEMRLSEPVPQTNAHESKEWYHASLTRAQAEHMLMRVPRDGAFLVRKRNEPNSYAISFRAEGKIKHCRVQQEGQTVMLGNSEFDSLVDLISYYEKHPLYRKMKLRYPINEEALEKIGTAEPDYGALYEGRNPGFYVEANPMPTFKCAVKALFDYKAQREDELTFIKSAIIQNVEKQEGGWWRGDYGGKKQLWFPSNYVEEMVNPVALEPEREHLDENSPLGDLLRGVLDVPACQIAIRPEGKNNRLFVFSISMASVAHWSLDVAADSQEELQDWVKKIREVAQTADARLTEGKIMERRKKIALELSELVVYCRPVPFDEEKIGTERACYRDMSSFPETKAEKYVNKAKGKKFLQYNRLQLSRIYPKGQRLDSSNYDPLPMWICGSQLVALNFQTPDKPMQMNQALFMTGRHCGYVLQPSTMRDEAFDPFDKSSLRGLEPCAISIEVLGARHLPKNGRGIVCPFVEIEVAGAEYDSTKQKTEFVVDNGLNPVWPAKPFHFQISNPEFAFLRFVVYEEDMFSDQNFLAQATFPVKGLKTGYRAVPLKNNYSEDLELASLLIKIDIFPAKENGDLSPFSGTSLRERGSDASGQLFHGRAREGSFESRYQQPFEDFRISQEHLADHFDSRERRAPRRTRVNGDNRL
  
Inhibitor
Name:
BDBM107352
Synonyms:
US9695200, 74
Type:
Small organic molecule
Emp. Form.:
C32H28N4O2
Mol. Mass.:
500.5903
SMILES:
CC(C)c1ccc(NC(=O)c2ccc(cc2)-c2c[nH]c3ncc(cc23)-c2cccc(NC(=O)C=C)c2)cc1
Structure:
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