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Target
Signal transducer and activator of transcription 1-alpha/beta
Ligand
BDBM50189926
Substrate
n/a
Meas. Tech.
ChEMBL_1591093 (CHEMBL3829061)
IC50
45900±n/a nM
Citation
 LaPorte, MG; Wang, Z; Colombo, R; Garzan, A; Peshkov, VA; Liang, M; Johnston, PA; Schurdak, ME; Sen, M; Camarco, DP; Hua, Y; Pollock, NI; Lazo, JS; Grandis, JR; Wipf, P; Huryn, DM Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors. Bioorg Med Chem Lett 26:3581-5 (2016) [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:
BDBM50189926
Synonyms:
CHEMBL3828159 | US10618914, Compound 6b | US11111253, Compound 6b
Type:
Small organic molecule
Emp. Form.:
C19H13ClN6S
Mol. Mass.:
392.865
SMILES:
Clc1cccc(c1)C1=Nn2c(SC1)nnc2-c1cc(n[nH]1)-c1ccccc1 |t:8|
Structure:
Search PDB for entries with ligand similarity: