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Target
Signal transducer and activator of transcription 1-alpha/beta
Ligand
BDBM50103748
Substrate
n/a
Meas. Tech.
ChEMBL_1436276 (CHEMBL3387776)
IC50
>50000±n/a nM
Citation
 LaPorte, MG; da Paz Lima, DJ; Zhang, F; Sen, M; Grandis, JR; Camarco, D; Hua, Y; Johnston, PA; Lazo, JS; Resnick, LO; Wipf, P; Huryn, 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:
BDBM50103748
Synonyms:
CHEMBL3337627
Type:
Small organic molecule
Emp. Form.:
C22H19N5O3
Mol. Mass.:
401.418
SMILES:
Cc1nc(Nc2nc(=O)c(Cc3ccccc3)c(C)[nH]2)nc2cc3OCOc3cc12
Structure:
Search PDB for entries with ligand similarity: