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Evaluation of a panel of furochromenones as the activator and inhibitor of tyrosinase

Chemical Biology and Drug Design

Using fungal tyrosinase-based in vitro biochemical assay, we obtained one compound ( 3k ) which could inhibit tyrosinase activity, and the other compound ( 4f ) that stimulated tyrosinase activity. In the present study, we investigated these compounds for their potential as antagonists or agonists of tyrosinase.

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Betulinic acid reduces inflammation in rats with sepsis?induced myocardial dysfunction by inhibiting TLR4/MyD88/NF??B signaling pathway

Chemical Biology and Drug Design

Then, cardiac function parameters were assessed using echocardiography, myocardial injury markers were quantified via biochemical assays, and myocardial histopathological injuries were observed through H&E staining.

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Variability in biological activity measurements reported in the drug discovery literature

Molecular Design

In the Compatibility Issues section the authors state: Looking beyond laboratory-to-laboratory variability of assays that are nominally the same, there are numerous reasons why literature results for different assays measured against the same “target” may not be comparable.

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SARS-CoV-2 main protease. Crowdsourcing, peptidomimetics and fragments

Molecular Design

The binding mode observed for 1 is shown below in Figure 1 and it’s likely that the groove region will need to be more fully exploited (this article will give you an idea of the sort of thing I have in mind) in order to achieve acceptable potency if the aldehyde warhead is replaced by nitrile. by forming a ring). by forming a ring).

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On quality criteria for covalent and degrader probes

Molecular Design

I’ll be taking a look at H2023 (Expanding Chemical Probe Space: Quality Criteria for Covalent and Degrader Probes) in this post and this article has also been discussed In The Pipeline. Carefully designed biochemical assays used in determining IC50 values can be well-suited as surrogates for k.inact/K.i measurements. (

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Article FDA Thank You Draft guidance on potency assays for CGT products garners extensive stakeholder input

Agency IQ

Assays are tests designed to assess various properties (like potency) of chemical or biological samples.

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Are fused tetrahydroquinolines interfering with your assay?

Molecular Design

I’ll be taking a look at B2023 (Fused Tetrahydroquinolines Are Interfering with Your Assay) in this post. The article has already been discussed in posts at Practical Fragments and In The Pipeline. It’s also worth noting that interference with read-out can also lead to false negatives.