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Target
Signal transducer and activator of transcription 1-alpha/beta
Ligand
BDBM196138
Substrate
n/a
Meas. Tech.
ChEMBL_1436276 (CHEMBL3387776)
IC50
5900±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:
BDBM196138
Synonyms:
US9211296, Table 7, Compd: 9
Type:
Small organic molecule
Emp. Form.:
C18H23N5
Mol. Mass.:
309.4087
SMILES:
CC1=CC(C)(C)N=C(Nc2nc(C)c3cc(C)cc(C)c3n2)N1 |t:1,6|
Structure:
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