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Indole

  • High-purity Indole
  • Extensive range of Indole
  • Ideal for drug discovery applications and organic synthesis
  • Fast delivery and expert support
Indole compounds are essential building blocks in pharmaceutical research. Our carefully curated selection offers diverse structures for SAR studies and lead optimization, ensuring quality and reliability for your projects.

Understanding Indole in Modern Chemistry

Explore the critical role of Indole in pharmaceutical development, medicinal chemistry research and organic chemistry.

Precision Chemistry

Precision Chemistry

Advanced synthesis techniques for superior quality compounds

Great Molecules for Chemical Diversity

Our catalogue of building blocks contains a diverse range of highly functionalised and decorated compounds. The 20 years of experience in supplying cutting-edge building blocks have given us the expertise to bring you the most exciting chemical motifs, adding chemical diversity to your projects.

Our diverse catalogue is tailored for medicinal chemistry, small molecule drug discovery and organic synthesis. Our unique range of Indole adds value to any research project.

We constantly add to our catalogue; the latest additions include a range of new Indole. We continue to bring you the latest and most exciting chemical compounds.

Quality Assurance

Quality Assurance

Every Indole product in our portfolio undergoes rigorous quality control testing. Our building blocks are supplied with the highest purity standards. We provide complete analytical characterisation, including:

  • ¹H and ¹³C NMR spectroscopy for structural verification
  • HPLC chromatograms confirming purity levels
  • Certificate of Analysis available.
  • Standard purity of 95%
  • Specific purity available upon request.

Diverse Applications

Diverse Applications

From oncology to neuroscience, enabling next-generation therapeutics

Over 4000 Indole in our catalogue
Found in over 45 FDA-approved drugs
95% of compounds available from stock

Indole products in our portfolio

Indole is among the most widely studied heterocyclic scaffolds in medicinal chemistry, present in numerous approved therapeutics and occurring naturally in the amino acid tryptophan, a range of alkaloids, and endogenous signalling molecules including serotonin and melatonin. Indoles offer a planar aromatic framework with a hydrogen-bond donor at the nitrogen and a nucleophilic C-3 position that provides a well-established point for functionalisation, alongside productive substitution at C-2 and across the benzene ring, allowing medicinal chemists to tune potency, selectivity, and physicochemical properties with considerable flexibility.

Indole-based drugs have outpaced other azaheterocycles in FDA approvals over the past decade, reflecting their exceptional versatility as pharmacophores across oncology, immunology, infectious disease, gastrointestinal disorders, and CNS programmes. Indoles support diverse binding modes, including hydrogen bond donation from the NH, π-stacking with aromatic residues, and hydrophobic burial of the bicyclic core within protein binding pockets, making it adaptable to a broad range of target classes including kinases, GPCRs, nuclear receptors, and complement proteases. Iptacopan (Fabhalta, Novartis) is an FDA-approved first-in-class oral complement Factor B inhibitor bearing a methoxy-methyl indole pharmacophore, approved in December 2023 as the first oral monotherapy for adults with paroxysmal nocturnal haemoglobinuria, acting proximally in the alternative complement pathway to control both intravascular and extravascular haemolysis.
Osimertinib (Tagrisso, AstraZeneca), approved by the FDA in 2015 as the first-in-class third-generation EGFR tyrosine kinase inhibitor for the treatment of EGFR T790M mutation-positive metastatic non-small cell lung cancer, incorporates a pendant 1-methylindol-3-yl group attached at the C-4 position of the central pyrimidine core, confirmed in the FDA label IUPAC name, where the unfused indole makes critical contacts within the mutant EGFR kinase domain and contributes directly to the selectivity for T790M and sensitising EGFR mutations over wild-type receptor.

Our range of Indoles features novel substitutions and the incorporation of synthetically tractable functional groups such as boronic acids and esters, amines, carboxylic acids, ketones, hydroxyls and halogens to enable expedient synthetic strategies. The full range can be found using the substructure feature of our Search tools.

Frequently Asked Questions

Common questions about our Indole products.

Indole is a bicyclic aromatic scaffold consisting of a benzene ring fused to a pyrrole, and it is among the most widely studied heterocycles in medicinal chemistry. It occurs naturally in the amino acid tryptophan and in endogenous signalling molecules including serotonin and melatonin. Indole-based drugs have outpaced other azaheterocycles in FDA approvals over the past decade, reflecting their versatility across oncology, immunology, infectious disease, and CNS programmes.

Indole supports several distinct binding modes. The NH acts as a hydrogen bond donor capable of engaging enzyme active sites, while the planar bicyclic core supports pi-stacking with aromatic residues and hydrophobic burial within protein binding pockets. The nucleophilic C-3 position provides an additional handle for functionalisation. Together, these features make indole adaptable to kinases, GPCRs, nuclear receptors, and complement proteases.
The most important positions for functionalisation on indole are the C-3 position, which is inherently nucleophilic and well established as a point for substitution, and C-2, which also supports productive derivatisation. Substitution across the benzene ring is accessible as well, allowing medicinal chemists to tune potency, selectivity, and physicochemical properties with considerable flexibility. Functional groups including boronic acids, amines, carboxylic acids, ketones, hydroxyls, and halogens are available on commercial indole building blocks.
Several FDA-approved drugs contain indole pharmacophores. Iptacopan (Fabhalta, Novartis) is a first-in-class oral complement Factor B inhibitor bearing a methoxy-methyl indole group, approved in December 2023 for paroxysmal nocturnal haemoglobinuria. Osimertinib (Tagrisso, AstraZeneca) is a third-generation EGFR tyrosine kinase inhibitor approved in 2015 for EGFR T790M mutation-positive metastatic non-small cell lung cancer, incorporating a 1-methylindol-3-yl group that contributes to its selectivity for mutant over wild-type EGFR.
Osimertinib incorporates a pendant 1-methylindol-3-yl group attached at the C-4 position of its central pyrimidine core. This indole group makes critical contacts within the mutant EGFR kinase domain and contributes directly to selectivity for T790M and sensitising EGFR mutations over the wild-type receptor. The combination of the indole pharmacophore with a covalent acrylamide warhead is what distinguishes osimertinib as a third-generation EGFR inhibitor.
Iptacopan (Fabhalta, Novartis) is a first-in-class oral complement Factor B inhibitor approved in December 2023 as the first oral monotherapy for adults with paroxysmal nocturnal haemoglobinuria. It bears a methoxy-methyl indole pharmacophore that enables potent inhibition of the alternative complement pathway, controlling both intravascular and extravascular haemolysis. This approval represents one of the most recent validations of the indole scaffold in an immunology programme.
Indole-based drugs have outpaced other azaheterocycles in FDA approvals over the past decade, which reflects their exceptional versatility as pharmacophores. The scaffold offers a unique combination of a hydrogen bond donor at the nitrogen, a reactive C-3 position, a planar aromatic surface for pi-stacking, and an amenable substitution profile across the benzene ring. This allows indole to be tuned for diverse target classes including kinases, GPCRs, and nuclear receptors across multiple therapeutic areas.
Yes. Indole is present in the amino acid tryptophan and in a range of alkaloids and endogenous signalling molecules. Serotonin and melatonin, both physiologically important neurotransmitters and hormones, are indole derivatives. This natural prevalence reflects the scaffold's compatibility with biological environments and helps explain why indole-containing compounds frequently show favourable pharmacokinetic and pharmacodynamic properties.

Still have questions?

Our technical support team is here to help with any inquiries about our Indole products.