TTI-101 [Ligand Id: 12268] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3392776 (C-188-9, Stat3 inhibitor c188-9, Stat3 inhibitor tti-101, Tti 101, Tti-101, TTI-101, TTI101) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| signal transducer and activator of transcription 3/Signal transducer and activator of transcription 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4026] [GtoPdb: 2994] [UniProtKB: P40763] | ||||||||
| ChEMBL | Binding affinity to full length STAT3 (unknown origin) by Surface plasmon resonance | B | 6.6 | pKd | 250 | nM | Kd | J Med Chem (2022) 65: 6710-6728 [PMID:35476936] |
| ChEMBL | Binding affinity to STAT3 (127 to 722 residues) (unknown origin) by microscale thermophoresis analysis | B | 8.33 | pKd | 4.7 | nM | Kd | Eur J Med Chem (2020) 187: 111922-111922 [PMID:31810784] |
| ChEMBL | Inhibition of STAT3 in human NB-4 cells assessed as inhibition of G-CSF induced STAT3 phosphorylation incubated for 60 mins by western blot assay | B | 5.08 | pIC50 | 8300 | nM | IC50 | Eur J Med Chem (2020) 187: 111922-111922 [PMID:31810784] |
| ChEMBL | Inhibition of STAT3 in human KG-1 cells assessed as inhibition of G-CSF induced STAT3 phosphorylation incubated for 60 mins by western blot assay | B | 5.39 | pIC50 | 4100 | nM | IC50 | Eur J Med Chem (2020) 187: 111922-111922 [PMID:31810784] |
| ChEMBL | Binding affinity to STAT3 (unknown origin) by SPR analysis | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (2021) 64: 8884-8915 [PMID:34170703] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
