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ChEMBL ligand: CHEMBL134561 (AR-100, Iclaprim, Ro-482622, RO 48-2622, RO-48-2622) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Dihydrofolate reductase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1809] [UniProtKB: P0ABQ4] | ||||||||
ChEMBL | Inhibition of Escherichia coli dihydrofolate reductase (DHFR) enzyme by trimethoprim (TMP) | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4217-4221 [PMID:14623005] |
Dihydrofolate reductase in S.aureus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1681620] [UniProtKB: P0A017] | ||||||||
ChEMBL | Inhibition of TMP-resistant Staphylococcus aureus DHFR F99Y mutant assessed as oxidation of NADPH using dihydrofolate as substrate pre-incubated for 10 mins before substrate addition by spectrophotometry | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5171-5176 [PMID:21831637] |
ChEMBL | Inhibition of Staphylococcus aureus DHFR assessed as oxidation of NADPH using dihydrofolate as substrate pre-incubated for 10 mins before substrate addition by spectrophotometry | B | 10.09 | pKi | 0.08 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5171-5176 [PMID:21831637] |
ChEMBL | Inhibition of Staphylococcus aureus DHFR using dihydrofolate as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis in presence of NADPH | B | 10.1 | pKi | 0.08 | nM | Ki | J Med Chem (2014) 57: 651-668 [PMID:24428639] |
ChEMBL | Inhibition of Staphylococcus aureus DHFR F98Y mutant by MTS assay | B | 7.57 | pIC50 | 27 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3825-3833 [PMID:20606069] |
ChEMBL | Inhibition of Staphylococcus aureus dihydrofolate reductase (DHFR) enzyme by trimethoprim (TMP) | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4217-4221 [PMID:14623005] |
ChEMBL | Inhibition of Staphylococcus aureus wild type recombinant DHFR by MTS assay | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3825-3833 [PMID:20606069] |
ChEMBL | Inhibition of Staphylococcus aureus wild type recombinant DHFR by MTS assay | B | 8.66 | pIC50 | 2.2 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3825-3833 [PMID:20606069] |
Dihydrofolate reductase in Pneumocystis carinii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1926] [UniProtKB: P16184] | ||||||||
ChEMBL | Inhibition of Pneumocystis carinii dihydrofolate reductase (DHFR) enzyme by trimethoprim (TMP) | B | 5.62 | pIC50 | 2400 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4217-4221 [PMID:14623005] |
dihydrofolate reductase/Dihydrofolate reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL202] [GtoPdb: 2603] [UniProtKB: P00374] | ||||||||
GtoPdb | - | - | 6.11 | pKi | 775 | nM | Ki | |
ChEMBL | Inhibition of human DHFR assessed as oxidation of NADPH using dihydrofolate as substrate pre-incubated for 10 mins before substrate addition by spectrophotometry | B | 6.11 | pKi | 775 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5171-5176 [PMID:21831637] |
ChEMBL | Inhibition of human DHFR using dihydrofolate as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis in presence of NADPH | B | 6.11 | pKi | 775 | nM | Ki | J Med Chem (2014) 57: 651-668 [PMID:24428639] |
ChEMBL | Inhibition of Human dihydrofolate reductase (DHFR) enzyme by Iclaprim | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4217-4221 [PMID:14623005] |
ChEMBL | Inhibition of Streptococcus pneumoniae dihydrofolate reductase (DHFR) enzyme by trimethoprim (TMP) | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4217-4221 [PMID:14623005] |
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]