azaindole-1

ROCK-IN-2 (Azaindole 1) is a selective and ATP-competitive ROCK inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2.

Nav1.2-IN-1 (compound 5i) is a 3-(1,2,3,6-tetrahydropyridine)-4-azaindole derivative that acts as a potent and selective Nav1.2 inhibitor. It effectively reduces the peak current of Nav1.2 with an IC50 of 7.79 μM. Nav1.2-IN-1 demonstrates antiepileptic activity and shows strong anticonvulsant effects with low neurotoxicity in a subcutaneous pentylenetetrazol (sc-PTZ) induced seizure model.

MethylCBI-azaindole-benzamide-MOM-Boc-ethylenediamine-D is a cleavable linker used in the formation of antibody-drug conjugates (ADCs), enabling the release of the cytotoxic drug upon internalization by target cells [1].

Vobramitamab (AEX-4089) is a humanized monoclonal antibody (mAb) targeting the B7-H3 antigen (CD276) which is conjugated to the prodrug seco-duocarmycin hydroxybenzamide azaindole (seco-DUBA) through a enzymatically cleavable peptide-based linker, thereby creating the investigational antibody-drug conjugate (ADC) known as MGC018.