fret assay

TMP778 is an effective and selective RORγt inverse agonist (IC50: 7 nM in FRET assay).

FMK 9a is an irreversible inhibitor of ATG4B with IC50 values of 80 and 73 nM in the TR-FRET and cellular-based LRA assays.

PX20606 trans racemate is an agonist of FXR (EC50s of 32 and 34 nM for FXR in FRET and M1H assay, respectively).

BAY1238097, a potent and selective bromodomain and extra-terminal motif (BET) inhibitor with anticancer activity, exhibits strong antiproliferative effects in AML (Acute Myeloid Leukemia) and MM (Multiple Myeloma) models. BAY1238097 is useful for studying advanced refractory malignancies.

GNE-049 is a highly selective and potent inhibitor designed to target the CREB-binding protein (CBP) with high affinity, exhibiting an IC50 of 1.1 nM for the suppression of BRET and BRD4 activity, which consequently blocks prostate cancer cell proliferation in both in vitro and in vivo models.

(1α,1'S,4β)-Lanabecestat is a Beta site APP Cleaving Enzyme 1 (BACE1) inhibitor with IC50 values of 2.2 nM in the TR-FRET assay and 0.28 nM in the sAPPp release assay.

AZD-5991 Racemate is the racemate of AZD-5991. (Rac)-AZD-5991 is a novel Mcl-1 inhibitor with IC50 <3 nM in FRET assay and induces upregulation of BCL2,BCL-XL, CMYC and MCL1 in AML cell lines.

GSK4028 is the enantiomeric negative control of GSK4027, a PCAF/GCN5 bromodomain chemical probe, with a pIC50 of 4.9 in a TR-FRET assay.

GSK 4027 is a PCAF/GCN5 bromodomain chemical probe. In a time-resolved fluorescence resonance energy transfer (TR-FRET) assay, it has a pIC50 of 7.4±0.11 for PCAF.

GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).

LZ-007 is an agonist of the Farnesoid X receptor (FXR), with an EC50 of 51 nM as determined by TR-FRET assay, and an EC50 of 76 nM in HepG2 cells. It exhibits favorable pharmacokinetic properties in SD rats and can improve metabolic dysfunction-associated steatohepatitis induced by high-fat diets and CCl4 in mice.

JNJ525 is an inhibitor of TNFα. JNJ525 inhibits protein function via an aggregation-based mechanism. JNJ525 prevents the formation of TNFα complexes with TNFR1 and TNFR2, the apparent IC50 values for the inhibition of complex formation are 1.2 ± 0.2 μM an

CAY10774 is an inhibitor of the protein-protein interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 (IC50= 15 nM in a homologous time-resolved fret (HTRF) assay).1It increases the activation of Jurkat cells expressing PD-1 in co-culture with artificial antigen-presenting cells (aAPCs) expressing PD-L1 (EC50= 6.6 μM in a reporter assay). CAY10774 increases surface expression of PD-1 on primary human CD4+and CD8+T cells co-cultured with aAPCs. 1.Konieczny, M., Musielak, B., Kocik, J., et al.Di-bromo-based small-molecule inhibitors of the PD-1/PD-L1 immune checkpointJ. Med. Chem.63(19)11271-11285(2020)

MProinhibitor 11b is an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (MPro; IC50= 0.04 μM in a TR-FRET assay).1It reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 cells (EC50= 0.72 μM). MProinhibitor 11b also reduces viral RNA copy numbers in the same model when used at concentrations ranging from 1.85 to 50 μM. 1.Dai, W., Zhang, B., Jiang, X.-M., et al.Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main proteaseScience368(6497)1331-1335(2020)

Cathepsin D and E FRET Substrate acetate is a fluorogenic substrate selectively cleaved by cathepsins D and E at the Phe-Phe amide bond, demonstrating no activity towards cathepsins B, H, or L. This specificity renders it essential for routine assays and mechanistic studies focusing on cathepsins E and D[1].

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.

RBP4 ligand-1 is a non-retinoid ligand for retinol-binding protein 4 (RBP4). It exhibits hRBP4SPA IC50 and RBP4-TTR FRET IC50 values of 0.23±0.11 μM and 0.13±0.12 μM, respectively, in radioligand binding and FRET assays. The measured concentration was 0.12 μM.

BAY1125976 is an allosteric inhibitor of Akt1 and Akt2 (IC50s of 5.2 and 18 nM, respectively, in a time-resolved FRET assay)

Iberdomide (CC-220) is a modulator of cereblon( IC50 value of 60 nM in a competitive TR-FRET assay).

hAChE-IN-1 (Compound 24) is a potent inhibitor of human acetylcholinesterase (hAChE), with an inhibition concentration half-maximum (IC50) of 1.09 μM, and inhibits tau-oligomerization with an effective concentration half-maximum (EC50) of 2.71 μM as determined by a cellular tau fluorescence resonance energy transfer (FRET) assay [1].

Keap1-Nrf2-IN-15 (Compound 24a) is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, with IC50 values of 77 nM in a fluorescence polarization (FP) assay and 2.5 nM in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay [1].

WAAG-3R is a bioactive peptide utilized in an ADAMTS-4 (Aggrecanase-1) assay, where aggrecanases, a subset of the ADAMTS (A disintegrin and metalloprotease with thrombospondin motifs) family, target aggrecan, a key structural component of cartilage. Notably, ADAMTS-4 is a principal aggrecanase in human osteoarthritic cartilage. The peptide's fluorescence resonance energy transfer (FRET) properties are evidenced by an excitation/emission (Ex/Em) spectrum of 340/420 nm.

Emavusertib (CA-4948) hydrochloride, a selective and potent IRAK4/FLT3 inhibitor, is designed for oral administration. It achieves an IC 50 of 57 nM against IRAK4 in a FRET kinase assay and demonstrates anti-tumor activity [1] [2] [3].