off-target

TCMDC-135051 is a potent and selective PfCLK3 protein kinase inhibitor demonstrating significant antiparasiticidal activity (EC50=320 nM) while exhibiting minimal off-target toxicity. It effectively hinders the transition from trophozoite to schizont, impairs transcription, and diminishes transmission to the mosquito vector.

DL-Mannitol is a osmotic diuretic, it may play a role in reducing off-target 68Ga-PSMA renal uptake

BRD20322 is a novel potent inhibitor of spCas9 that disrupts spCas9-DNA binding and exerts dose and temporal control of spCas9 in human cell lines. It reduces off-target DNA editing events, enhancing the precision and safety of CRISPR-Cas9 gene editing.

ERK-IN-2, an ERK2 inhibitor, exhibits an IC50 value of 1.8 nM. At doses greater than 10 μM, it may induce off-target toxicity and or activity [1].

Vc-MMAD, a drug-linker conjugate for Antibody-Drug Conjugates (ADCs), combines the ADC linker Val-Cit (Valine-Citrulline) with the potent tubulin inhibitor MMAD. This compound leverages the targeting capability of ADCs to deliver the cytotoxic agent MMAD specifically to cancer cells, enhancing therapeutic efficacy while minimizing off-target effects.

PTC299 ((4-chlorophenyl) (1S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydropyrido[3,4-b]indole-2-carboxylate) is an orally active inhibitor of VEGFA mRNA translation and selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydrolactate dehydrogenase (DHODH).

GNE-4997 is a potent and selective inhibitor of the interleukin-2-inducible T-cell kinase (Ki: 0.09 nM). The correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity.

Antiviralagent 59 (compound 58) is a selective antiviral agent with drug-like properties, capable of inhibiting a broad spectrum of filoviruses. It demonstrates low off-target activity and inhibitory effects against replicative forms of Ebola virus (EBOV), Sudan virus (SUDV), and Marburg virus (MARV).

(3S, 4S)-PF-06459988 is the less active S enantiomer of PF-06459988, a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR), exhibiting excellent selectivity against EGFR wild-type due to its minimally reactive electrophile, reducing off-target labeling likelihood.

UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT5AR with a more restricted off-target profile and decreased assay liabilities compared to the commercial antagonist SB-699551. UCSF678 is a selective probe for studying the function of the 5-HT5AR [1].

UCSF686 is a UCSF678 analog that is devoid of the 5-HT5A potency, while preserving the off-target affinity (5-HT1A, 5-HT2B and 5-HT7). UCSF686 is recommended as a control compound when using UCSF678 for probing 5-HT5A-dependent activities in cultures and in vivo [1].

TCMDC-135051 hydrochloride is a potent, highly selective, low off-target toxicity inhibitor of the protein kinase PfCLK3. TCMDC-135051 hydrochloride blocks the trophozoite to lysosome transition, disrupts transcription and inhibits transmission to mosquito vectors, exhibiting an antiparasitic effect with an EC50 value of 320 nM.

TCMDC-135051 TFA is a potent, highly selective, low off-target toxicity protein kinase PfCLK3 inhibitor that exhibits antiparasitic effects with an EC50 value of 320 nM. TCMDC-135051 TFA blocks the trophozoite to lytic transition, disrupts transcription and inhibits transmission to mosquito vectors.

AK-42 is a novel potent and specific inhibitor of CLC-2, displaying unprecedented selectivity over CLC-1, the closest CLC-2 homolog, and exhibiting no off-target engagement against a panel of 61 common channels, receptors, and transporters expressed in brain tissue.

ERK-IN-2 free base, an inhibitor of ERK2, demonstrates potent efficacy with an IC50 value of 1.8 nM. However, doses exceeding 10 μM may result in off-target toxicity and or activity.

Olgotrelvir is an antiviral agent [1]. It inhibits viral replication by targeting key viral enzymes, thereby reducing the viral load in infected cells. The compound exhibits specificity for its target enzymes, which minimizes off-target effects and enhances its therapeutic profile. Clinical studies demonstrate its efficacy against a range of viral pathogens.

Isoguaiacin, a natural product [1], exhibits (hass) the potential to be (to exist as) an (a) effective pharmacological agent due to its (its) ability to inhibit (the inhibition of) mushroom tyrosinase. This (The) inhibition is (taking place) in a manner that demonstrates greater (a higher) selectivity towards mushroom tyrosinase compared to human tyrosinase, suggesting a reduced (a lower) risk of off-target effects in humans. Additionally, isoguaiacin shows (displays) promising (promising) activity against (in combating) certain cancer cell lines, further affirming its potential as (an) anticancer agent.

Amidate-VC-PAB-MMAF, a cleavable ADC linker (Amidate-VC-PAB) combined with a potent tubulin polymerization inhibitor (MMAF), is utilized in the synthesis of antibody-drug conjugates (ADCs) to decrease off-target cytotoxicity[1].

Vodobatinib (K-0706) is a novel 3rd generation (3G) TKI effective against wild-type and mutated BCR-ABL1 with limited off-target activity.