ChEMBL ligand: CHEMBL260015
transforming growth factor beta receptor 1/TGF-beta receptor type I in Human [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897] There should be some charts here, you may need to enable JavaScript!
transforming growth factor beta receptor 2/TGF-beta receptor type II in Human [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
transforming growth factor beta receptor 1/TGF-beta receptor type I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
GtoPdb	-	-	7.42	pKi	38	nM	Ki	Mol Cancer Ther (2008) 7: 829-40 [PMID:18413796]
ChEMBL	Inhibition of TbetaR-1 (unknown origin) assessed as inhibition constant by ELISA assay	B	7.42	pKi	38	nM	Ki	Eur J Med Chem (2020) 191: 112154-112154 [PMID:32092587]
ChEMBL	Inhibition of TGFbetaR1 in human primary T-cells assessed as TGFbeta-stimulated PSMAD phosphorylation preincubated for 1 hr followed by TGFbeta addition measured after 90 mins by Alpha screen assay	B	6.43	pIC50	370	nM	IC50	Bioorg Med Chem (2018) 26: 1026-1034 [PMID:29422332]
ChEMBL	Inhibition of TGFbeta type receptor 1 ALK5 (T204D) expressed in Sf9 cells	B	7.16	pIC50	69	nM	IC50	J Med Chem (2008) 51: 2302-2306 [PMID:18314943]
ChEMBL	Inhibition of human His-tagged TGFbetaR1 T204D mutant expressed in Sf9 insect cells after 1 hr by HTRF assay	B	8.43	pIC50	3.7	nM	IC50	Bioorg Med Chem (2018) 26: 1026-1034 [PMID:29422332]
transforming growth factor beta receptor 2/TGF-beta receptor type II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173]
GtoPdb	-	-	6.52	pKi	300	nM	Ki	Mol Cancer Ther (2008) 7: 829-40 [PMID:18413796]
ChEMBL	Inhibition of TbetaR-2 (unknown origin) assessed as inhibition constant by ELISA assay	B	6.52	pKi	300	nM	Ki	Eur J Med Chem (2020) 191: 112154-112154 [PMID:32092587]
ChEMBL	Inhibition of wild type His-tagged TGFbetaR2 (unknown origin) after 1 hr by HTRF assay	B	6.72	pIC50	190	nM	IC50	Bioorg Med Chem (2018) 26: 1026-1034 [PMID:29422332]

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]