ChEMBL ligand: CHEMBL1201746 (Folotyn, NSC-754230, PDX, Pralatrexate, Pralatrexato)
dihydrofolate reductase/Dihydrofolate reductase in Human [ChEMBL: CHEMBL202] [GtoPdb: 2603] [UniProtKB: P00374] There should be some charts here, you may need to enable JavaScript!
folate receptor alpha/Folate receptor alpha in Human [ChEMBL: CHEMBL2121] [GtoPdb: 3212] [UniProtKB: P15328] There should be some charts here, you may need to enable JavaScript!
Reduced folate transporter 1/Folate transporter 1 in Human [ChEMBL: CHEMBL4833] [GtoPdb: 1014] [UniProtKB: P41440] There should be some charts here, you may need to enable JavaScript!
Proton-coupled folate transporter in Human [ChEMBL: CHEMBL1795188] [GtoPdb: 1213] [UniProtKB: Q96NT5] 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
dihydrofolate reductase/Dihydrofolate reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL202] [GtoPdb: 2603] [UniProtKB: P00374]
GtoPdb	-	-	7.35	pKi	45	nM	Ki	Cancer Chemother Pharmacol (2009) 64: 993-9 [PMID:19221750]
ChEMBL	Inhibition of DHFR (unknown origin) at pH 6.7	B	10.87	pKi	0.01	nM	Ki	Eur J Med Chem (2021) 214: 113218-113218 [PMID:33540357]
folate receptor alpha/Folate receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2121] [GtoPdb: 3212] [UniProtKB: P15328]
ChEMBL	Binding affinity to human FR-alpha receptor expressed in Chinese hamster RT16 cells assessed as antiproliferative activity measured as reduction in cell viability after 96 hrs in presence of folic acid by Cell-Titer Blue assay	B	6	pIC50	>1000	nM	IC50	J Med Chem (2018) 61: 2027-2040 [PMID:29425443]
ChEMBL	Binding affinity to human FR-alpha receptor expressed in Chinese hamster RT16 cells assessed as antiproliferative activity measured as reduction in cell viability after 96 hrs by Cell-Titer Blue assay	B	6.77	pIC50	168	nM	IC50	J Med Chem (2018) 61: 2027-2040 [PMID:29425443]
Reduced folate transporter 1/Folate transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4833] [GtoPdb: 1014] [UniProtKB: P41440]
ChEMBL	Binding affinity to human RFC expressed in Chinese hamster PC43-10 cells assessed as antiproliferative activity measured as reduction in cell viability after 96 hrs by Cell-Titer Blue assay	B	9.16	pIC50	0.69	nM	IC50	J Med Chem (2018) 61: 2027-2040 [PMID:29425443]
Proton-coupled folate transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795188] [GtoPdb: 1213] [UniProtKB: Q96NT5]
ChEMBL	Binding affinity to human PCFT expressed in Chinese hamster R2/PCFT4 cells assessed as antiproliferative activity measured as reduction in cell viability after 96 hrs by Cell-Titer Blue assay	B	7.24	pIC50	57	nM	IC50	J Med Chem (2018) 61: 2027-2040 [PMID:29425443]

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]