Target
Signal transducer and activator of transcription 1-alpha/beta
Ligand
BDBM50103759
Substrate
n/a
Meas. Tech.
ChEMBL_1436276 (CHEMBL3387776)
IC50
12100±n/a nM
Citation
 LaPorte, MGda Paz Lima, DJZhang, FSen, MGrandis, JRCamarco, DHua, YJohnston, PALazo, JSResnick, LOWipf, PHuryn, DM 2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway. Bioorg Med Chem Lett 24:5081-5 (2014) [PubMed]  Article 
Target
Name:
Signal transducer and activator of transcription 1-alpha/beta
Synonyms:
STAT1 | STAT1_HUMAN | Signal transducer and activator of transcription 1-alpha/beta | Transcription Factor STAT1 | Transcription factor ISGF-3 components p91/p84 | signal transducer and activator of transcription 1 isoform alpha
Type:
Cytosolic Transcription Factor
Mol. Mass.:
87327.69
Organism:
Homo sapiens (Human)
Description:
Stat1 was expressed in sf9 cells from a baculovirus encoding the recombinant proteins. Stat1 dimer binds to DNA.
Residue:
750
Sequence:
MSQWYELQQLDSKFLEQVHQLYDDSFPMEIRQYLAQWLEKQDWEHAANDVSFATIRFHDLLSQLDDQYSRFSLENNFLLQHNIRKSKRNLQDNFQEDPIQMSMIIYSCLKEERKILENAQRFNQAQSGNIQSTVMLDKQKELDSKVRNVKDKVMCIEHEIKSLEDLQDEYDFKCKTLQNREHETNGVAKSDQKQEQLLLKKMYLMLDNKRKEVVHKIIELLNVTELTQNALINDELVEWKRRQQSACIGGPPNACLDQLQNWFTIVAESLQQVRQQLKKLEELEQKYTYEHDPITKNKQVLWDRTFSLFQQLIQSSFVVERQPCMPTHPQRPLVLKTGVQFTVKLRLLVKLQELNYNLKVKVLFDKDVNERNTVKGFRKFNILGTHTKVMNMEESTNGSLAAEFRHLQLKEQKNAGTRTNEGPLIVTEELHSLSFETQLCQPGLVIDLETTSLPVVVISNVSQLPSGWASILWYNMLVAEPRNLSFFLTPPCARWAQLSEVLSWQFSSVTKRGLNVDQLNMLGEKLLGPNASPDGLIPWTRFCKENINDKNFPFWLWIESILELIKKHLLPLWNDGCIMGFISKERERALLKDQQPGTFLLRFSESSREGAITFTWVERSQNGGEPDFHAVEPYTKKELSAVTFPDIIRNYKVMAAENIPENPLKYLYPNIDKDHAFGKYYSRPKEAPEPMELDGPKGTGYIKTELISVSEVHPSRLQTTDNLLPMSPEEFDEVSRIVGSVEFDSMMNTV
  
Inhibitor
Name:
BDBM50103759
Synonyms:
CHEMBL1603850 | DNDI1417175
Type:
Small organic molecule
Emp. Form.:
C16H17N5O
Mol. Mass.:
295.3391
SMILES:
Cc1cc(C)c2nc(Nc3nc(C)cc(O)n3)nc(C)c2c1
Structure:
Search PDB for entries with ligand similarity: