analogue

Filgotinib analogue isa a structurally analogue of Filgotinib and can be used in life science related research.

Phentolamine Analogue 1 is a nonselective α-adrenergic antagonist, similar to phentolamine.

Pilaralisib analogue (XL147 analogue) is a selective and reversible class I PI3K inhibitor targeting PI3Kα/δ/γ.

CPI-455 analogue (CPI-455 analogue) is an analogue of CPI-455 which is a KDM5 inhibitor.

Hymenialdisine Analogue #1 is the indole derivative of Hymenialdisine, a potent inhibitor of a variety of kinases including MEK-1, GSK-3Β, and CKI. It also exhibits inhibition of the G2 cell cycle checkpoint at the micromolar concentrations.

PI3K-IN-1 (Voxtalisib Analogue) is a dual inhibitor of mTOR/PI3K, mostly for p110γ , also inhibits DNA-PK and mTOR.

IDO5L (INCB024360 analogue) is an effective IDO1 inhibitor(IC50=10 nM).

GLPG0634 analog (GLPG0634 analogue) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.

ONO-4059 analog (ONO-WG-307)ue is an analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with IC50 of 23.9 nM. Phase 1.

Macitentan n-butyl analogue, a derivative of Macitentan, functions as an orally active dual antagonist targeting both endothelin ETA and ETB receptors. This compound shows promise for treating idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH), leveraging its non-peptide structure for potential therapeutic applications.

Clofarabine (Clofarex)m, a second generation purine nucleoside analog with antineoplastic activity, inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.

Acipimox (K-9321) is a niacin derivative and nicotinic acid analog with activity as a hypolipidemic agent. Acipimox has special application for the treatment of hyperlipidemia in non-insulin-dependent diabetic patients.

Stavudine (BMY-27857), a nucleoside reverse transcriptase inhibitor analog of thymidine, has activity against HIV.

Glufosinate ammonium is a phosphinic acid analog of glutamic acid and an herbicide with neurotoxic activity. It is converted by plant cells into PT (L-phosphinothricin).

Adefovir dipivoxil (GS 0840) is a dipivoxil formulation of adefovir, a nucleoside reverse transcriptase inhibitor analog of adenosine with activity against hepatitis B virus (HBV), herpes virus, and human immunodeficiency virus (HIV).

D-(+)-Fucose is a non-metabolizable analog of l-arabinose and an inducer of β-methylgalactoside permease. It inhibits the induction of the l-arabinose manipulator and blocks the growth of Escherichia coli B/r on mineral salts medium with l-arabinose.

2,6-Dichlorodiphenylamine, an analogue of Diclofenac Sodium, exhibits anti-Candida albicans activity. Diclofenac Sodium, a potent and nonselective COX inhibitor, has IC50 values of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells. [1]. Makoto Urai, et al. Potent Drugs That Attenuate anti-Candida albicans Activity of Fluconazole and Their Possible Mechanisms of Action. J Infect Chemother. 2014 Oct;20(10):612-5.

3-Bromopyruvic acid (Hexokinase II Inhibitor II, 3-BP) is a hexokinase II inhibitor with Ki of 2.4 mM for glycolysis/hexokinase inhibition. It is inhibitor of tumour cell energy metabolism and chemopotentiator of platinum drugs.

2-Chloroadenosine (CADO) is a metabolically stable analog of adenosine that binds to adenosine A1, A2A, and A3 receptors( Ki:300, 80, and 1,900 nM, respectively)

Azvudine (FNC) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine inhibits NRTI-resistant viral strains. Azvudine exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM).

Carboprost tromethamine, a synthetic 15-methyl analogue of prostaglandin F2α, effectively promotes uterine contractions and significantly reduces bleeding during and post-delivery.

Iobenguane sulfate (MIBG sulfate) is a high-affinity substrate for cholera toxin that disrupts cellular mono(ADP-ribosylation). Radioiodinated Iobenguane sulfate is used clinically as a tumor-targeted radiopharmaceutical for diagnosing and treating adrenergic tumors.

Brodimoprim is an inhibitor of dihydrofolate reductase(DHFR). Brodimoprim is also a long-acting broad-spectrum antibacterial agent characterized by a good pharmacokinetic profile.

KRCA-0008 is an effective and specific ALK/Ack1 inhibitor (IC50: 12/4 nM); displays drug-like properties without hERG liability.