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Target
3-phosphoinositide-dependent protein kinase 1
Ligand
BDBM16673
Substrate
n/a
Meas. Tech.
ChEMBL_655516 (CHEMBL1244560)
Kd
>10000±n/a nM
Citation
 Zarrinkar, PP; Gunawardane, RN; Cramer, MD; Gardner, MF; Brigham, D; Belli, B; Karaman, MW; Pratz, KW; Pallares, G; Chao, Q; Sprankle, KG; Patel, HK; Levis, M; Armstrong, RC; James, J; Bhagwat, SS AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood 114:2984-92 (2009) [PubMed]  Article 
Target
Name:
3-phosphoinositide-dependent protein kinase 1
Synonyms:
3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) | 3-phosphoinositide dependent protein kinase-1 | 3-phosphoinositide-dependent protein kinase 1 | 3-phosphoinositide-dependent protein kinase 1 (PDK) | 3-phosphoinositide-dependent protein kinase 1 (PDK-1) | 3-phosphoinositide-dependent protein kinase 1 (PDK1)(Δ1-50) | Isoform 2 of 3-phosphoinositide-dependent protein kinase 1 | PDK1 | PDPK1 | PDPK1_HUMAN | Phosphoinositide-dependent protein kinase 1 (PDK1) | Pyruvate dehydrogenase kinase isoenzyme 1 (PDK1) | hPDK1
Type:
Enzyme
Mol. Mass.:
63157.65
Organism:
Homo sapiens (Human)
Description:
O15530
Residue:
556
Sequence:
MARTTSQLYDAVPIQSSVVLCSCPSPSMVRTQTESSTPPGIPGGSRQGPAMDGTAAEPRPGAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIKENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGELLKYIRKIGSFDETCTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARANSFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYDFPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLTAYLPAMSEDDEDCYGNYDNLLSQFGCMQVSSSSSSHSLSASDTGLPQRSGSNIEQYIHDLDSNSFELDLQFSEDEKRLLLEKQAGGNPWHQFVENNLILKMGPVDKRKGLFARRRQLLLTEGPHLYYVDPVNKVLKGEIPWSQELRPEAKNFKTFFVHTPNRTYYLMDPSGNAHKWCRKIQEVWRQRYQSHPDAAVQ
  
Inhibitor
Name:
BDBM16673
Synonyms:
4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide | 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methyl-picolinamide;tosylic acid | BAY 43-9006 | BAY 439006 | BAY439006 | CHEMBL1336 | Hit compound, 8 | Nexavar | Sorafenib | Sorafenib, 4 | US10183928, Sorafenib | US10202365, Compound Sorafenib | US10227329, Compound Sorafenib | US10584114, Compound Sorafenib | US10774070, Compound Sorafenib | US10980809, Example Sorafenib | US11279688, Compound Sorafenib | US11505527, Compound Sorafenib | US9029401, Sorafenib | US9469639, Sorafenib | US9902709, Comparative example 1 | Xarelto | cid_216239
Type:
Small organic molecule
Emp. Form.:
C21H16ClF3N4O3
Mol. Mass.:
464.825
SMILES:
CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)cc2)ccn1
Structure:
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