Chemical Biology and Drug Design

MAY 17, 2024

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.

Biochemical Assays 100

Biochemical Assays Regulations Production Research 100

Molecular Design

JULY 6, 2025

If this seems a bit extreme it’s worth pointing out that to accurately measure an IC 50 value of 10 μM requires that the compound be soluble, while neither aggregating nor interfering with assay read-out, at a concentration of 100 μM.

Biochemical Assays 71

Biochemical Assays Biophysical Assays Targeted Protein Degradation Drugs 71

ASPET

DECEMBER 21, 2023

Based on the druggability of DR3penA, we sought to investigate its effects on respirable particulate silicon dioxide (SiO 2 )- and soluble chemical paraquat (PQ)-induced pulmonary fibrosis in this study by using western blot, RT-qPCR, immunofluorescence, H&E and Masson staining, immunohistochemistry and serum biochemical assays.

Biochemical Assays 100

Biochemical Assays Small Molecule Disease Regulations 100

Chemical Biology and Drug Design

JANUARY 23, 2024

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.

Biochemical Assays 100

Biochemical Assays Protein Expression Drugs Research 100

Sygnature Discovery

MARCH 14, 2025

Advanced Automation in Sygnature Discoverys HTS System Our high throughput screening system, developed by HighRes Biosolutions, is designed for versatility, accommodating both cell and biochemical assays. Central to our automation is the Echo acoustic dispensing technology, ensuring highly accurate compound delivery.

Biochemical Assays 52

Biochemical Assays Fragment Screening Computational Chemistry Assay Development 52

Broad Institute

JUNE 16, 2025

Today, she uses induced pluripotent stem (iPS) cells, mouse models, biochemical assays, and high-throughput screening to study the role of TMED cargo receptors in Alzheimer’s disease. I love the idea of studying biology at its core, where the same basic principles can apply across different systems.”

Research 64

Research Biochemical Assays Disease Pharmacy 64

Drug Target Review

NOVEMBER 1, 2023

We often screen using a biochemical assay, but we can conduct cell-based screening as well. For fragment screening, we can screen with biophysical methods, such as thermal shift assays or, you may have heard about Surface Plasmon Resonance (SPR) which is a very sensitive biophysical technique used for fragment screening.

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Fragment Screening Biochemical Assays Small Molecule Biophysical Assays 96

Molecular Design

SEPTEMBER 18, 2024

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.

Biochemical Assays 68

Biochemical Assays Drugs Biophysical Assays Cell Based Assays 68

Molecular Design

JULY 18, 2020

One point that comes out of Pat’s post is that it’s difficult to establish structure-activity relationships for low affinity ligands with a conventional biochemical assay. This is one reason that biophysical detection of binding using methods such as surface plasmon resonance (SPR) are favored in fragment-based lead discovery.

Biochemical Assays 52

Biochemical Assays Fragment Screening Pharmacokinetics Drugs 52

PerkinElmer

FEBRUARY 18, 2021

Biochemical assays have the highest success rate. The top 20 Pharma are moving away from proteins in biochemical assays and overexpressed targets in simple cell lines toward more physiologically relevant assays using primary cells, cocultures, 3-D cell systems, or organoids. Biologics are booming. Think again.

Biochemical Assays 52

Biochemical Assays Drugs Small Molecule Pharma Companies 52

The Strateos Blog: Drug Discovery

DECEMBER 13, 2021

Additionally, Strateos' Senior Director of R&D Strategy, Daniel Rines, Ph.D.,  will be participating in a panel discussion during SLAS2022 February 7th 4:30-6:00pm EST alongside other thought leaders to discuss artificial intelligence in labs now and in the future.

Biochemical Assays 52

Biochemical Assays Small Molecule Laboratories Science 52

Molecular Design

DECEMBER 19, 2023

Carefully designed biochemical assays used in determining IC50 values can be well-suited as surrogates for k.inact/K.i [The labor-intensive nature of the measurements is not a valid justification for a failure to measure k.inact and K.i values for a covalent chemical probe.] measurements. ( values for the inhibitor.]

Small Molecule 65

Small Molecule Biochemical Assays Cell Based Assays Drugs 65

Drug Target Review

JANUARY 5, 2024

Å resolution) 6 is now being targeted for small molecule inhibitor discovery and development, by exploiting emergent computational tools to identify potential candidate compounds in silico and then test these predicted inhibitors in in vitro biochemical assays.

Small Molecule 59

Small Molecule Drugs Biochemical Assays Regulations 59

Practical Cheminformatics

AUGUST 3, 2023

Initially, I would recommend aqueous solubility, membrane permeability, in vitro metabolic stability, and biochemical assays. Focus benchmarking efforts on simple, robust, relevant, clearly defined endpoints. These endpoints are reproducible, relatively inexpensive, and can provide reasonably large datasets.

Drugs 84

Drugs Biochemical Assays Metabolic Stability Screening Hits 84

Molecular Design

DECEMBER 6, 2023

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.

Biochemical Assays 52

Biochemical Assays Small Molecule Drugs Laboratories 52

Agency IQ

JUNE 26, 2023

Further, footnote 7 in the document explains: “Examples of such clinical laboratory tests are commonly used and well understood biochemical assays (e.g., As the 2014 definitions document states (footnote 6): “Uses of diagnostic devices that are suggested but not required in therapeutic product labeling are not considered essential.””

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FDA Laboratories Clinical Trials Science 40

Agency IQ

APRIL 12, 2024

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

Production 40

Production FDA Therapies Biochemical Assays 40

Drug Target Review

DECEMBER 8, 2023

In our project, we used biochemical assays to identify which proteins interact with Rnf43.” “We wanted to know how Rnf43 works, and also what – in turn – controls Rnf43 and helps it to regulate Wnt signalling.” A crucial partner of Rnf43 turned out to be the protein Daam1.

Biochemical Assays 59

Biochemical Assays Regulations Science Laboratories 59

Covalent Modifiers

MAY 2, 2025

Glecirasib exhibited high potency against KRAS G12C, along with a high level of selectivity over the wild-type KRAS, HRAS, and NRAS in biochemical assays. In the current study, we report the preclinical characteristics of a specific KRAS p.G12C covalent inhibitor, glecirasib.

Biochemical Assays 162

Biochemical Assays Clinical Trials Trials Treatment 162

Chemical Biology and Drug Design

APRIL 3, 2025

Subsequent rounds of in silico docking, medicinal chemistry optimization, and biochemical assays were performed to increase its potency and selectivity for SRPK3. Six top compounds were identified that displayed single digit micromolar IC 50 values in SRPK3 activity assays and negligible inhibition of SRPK1 or SRPK2.

Biochemical Assays 100

Biochemical Assays Disease Drugs Research 100