Query String: AICAR
- Wall, M; Shim, JH; Benkovic, SJ A multisubstrate adduct inhibitor of AICAR transformylase. J Med Chem 42: 3421-4 (1999)
- Capps, KJ; Humiston, J; Dominique, R; Hwang, I; Boger, DL Discovery of AICAR Tfase inhibitors that disrupt requisite enzyme dimerization. Bioorg Med Chem Lett 15: 2840-4 (2005)
- Spurr, IB; Birts, CN; Cuda, F; Benkovic, SJ; Blaydes, JP; Tavassoli, A Targeting Tumour Proliferation with a Small-Molecule Inhibitor of AICAR Transformylase Homodimerization. Chembiochem 13: 1628-34 (2012)
- Boger, DL; Marsilje, TH; Castro, RA; Hedrick, MP; Jin, Q; Baker, SJ; Shim, JH; Benkovic, SJ Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase. Bioorg Med Chem Lett 10: 1471-5 (2000)
- ChEMBL_28413 (CHEMBL642457) Inhibitory activity against AICAR formyltransferase
- ChEMBL_28428 (CHEMBL875660) Inhibitory activity against AICAR formyltransferase
- ChEMBL_28429 (CHEMBL642471) Binding affinity towards AICAR formyltransferase
- ChEMBL_302287 (CHEMBL830304) Inhibition constant against AICAR formyltransferase
- ChEMBL_430370 (CHEMBL914875) Inhibition of human AICAR Tfase
- ChEMBL_1988115 (CHEMBL4621662) Inhibition of AICAR transformylase (unknown origin)
- ChEMBL_353451 (CHEMBL861363) Inhibition of human recombinant AICAR Tfase
- ChEBML_28408 Compound was tested for inhibition of AICAR formyltransferase
- ChEBML_28410 Inhibitory activity against AICAR formyltransferase of Lactobacillus casei
- ChEBML_28412 Concentration inhibiting AICAR formyltransferase enzyme of Lactobacillus casei
- ChEMBL_28409 (CHEMBL636972) Inhibition of AICAR formyltransferase in Lactobacillus casei
- ChEMBL_28411 (CHEMBL642455) Inhibitory concentration against Lactobacillus casei AICAR formyltransferase
- ChEBML_28418 Inhibition activity against AICAR formyltransferase determined against MOLT-4
- ChEMBL_28414 (CHEMBL642458) Inhibition activity against AICAR formyltransferase from hog liver
- ChEMBL_28424 (CHEMBL642467) Inhibition activity against AICAR formyltransferase determined against L cell
- ChEMBL_28426 (CHEMBL642469) Inhibition activity against AICAR formyltransferase determined against L cell
- ChEMBL_28427 (CHEMBL642470) Inhibition activity against AICAR formyltransferase determined against MOLT-4
- ChEBML_28421 Inhibition of AICAR formyltransferase from extract of Manca human lymphoma cells
- AICAR Tfase Inhibition Assay Recombinant human AICAR Tfase was used in the inhibition assay. The reaction was monitored at 298 nm by measuring the increase in absorbance corresponding to the formation of THF. The THF was generated in the transfer reaction of the formyl group from cofactor to AICAR to produce 5-formyl-AICAR. Double reciprocal plots were used to determine the Ki values.
- ChEBML_28431 In vitro inhibitory activity against MOLT-4 T-cell leukemia cell AICAR transformylase
- ChEMBL_28425 (CHEMBL642468) Triglutamyl homologue inhibition activity against AICAR formyltransferase was determined against L cell
- ChEMBL_28417 (CHEMBL642461) Hexaglutamyl homologue inhibition activity against the AICAR formyltransferase was determined against MOLT-4
- ChEMBL_28423 (CHEMBL642466) Hexaglutamyl homologue inhibition activity against the AICAR formyltransferase was determined against L cell
- ChEBML_28407 Compound was evaluated for the inhibition of Aminoimidazole carboxamide ribonucleotide formyl transferase (AICAR) with (6R) tetrahydrofolate as substrate
- AICAR Tfase Inhibition Assay The human ATIC enzyme was used for the inhibition assay. The assay buffer was flushed with nitrogen to minimize oxidization of cofactor 10-f-THF. The reaction was initiated by adding the substrate AICAR to reaction mixtures containing ATIC, test compounds, and different concentrations of cofactor. Using a SpectraMax Plus384 microplate reader, the reaction was monitored at 298 nm by measuring the increase in absorbance corresponding to the formation of THF. The THF was generated in the transfer reaction of the formyl group from cofactor to AICAR to produce 5-formyl-AICAR. IC50 values were measured from dose-response curves.
- ChEBML_1717838 Inhibition of recombinant human AICARFTase using AICAR as substrate incubated at 37 degC for 30 mins measured after overnight incubation at 4 degC
