Cromoglicic acid is a compound with multifaceted bioactivities and properties, showcasing potential in various biological contexts. It has a binding constant of Log K' = 1.07 against human serum albumin (HSA), suggesting its ability to bind and be transported by this protein in the body. It is highly acidic with pKa values below 2.0 and exhibits a dissociation constant (pKa) of 1.9. In human pharmacokinetics, it demonstrates a fraction unbound in plasma logFu of 0.0 and a volume of distribution at steady state (Vdss) of 0.32 L.kg-1, with an unbound Cmax of 0.192 µM.
Cromoglicic acid also displays bioactivities as an inhibitor of:
- Lamin A splicing (potency: 707.9 nM).
- Tyrosyl-DNA Phosphodiesterase (TDP1) (potency: 1778.3 nM).
- Various viral activities, including Marburg Virus, Lassa Virus, and SARS-CoV-2, although with varying potencies for each virus.
- Plasmodium falciparum proliferation (potency ranging from 0.7 to 37.6 nM).
- Human Apurinic/apyrimidinic Endonuclease 1 (APE1) (potency: 631.0 nM).
In addition to these bioactivities, Cromoglicic acid acts as an agonist at human GPR35, showing EC50 values in various assays, such as 210.0 nM in Ca+2 release and 520.0 nM in DMR assays. It exhibits a competitive binding affinity to Nluc-fused human GPR35 with a Ki value of 2970.0 nM.
Regarding safety and absorption, Cromoglicic acid has a hepatic side effect (HepSE) score of 1.0, indicating a risk for liver disease, without observable acute hepatotoxicity. It is moderately absorbed in the human intestine with a log10(%HIA) of approximately 1.021 and shows minimal inhibition of the Bile Salt Export Pump (BSEP), with an IC50 value greater than 1,000,000 nM.
Cromoglicic acid also impacts various biological parameters, influencing liver enzymes, kidney function markers, electrolytes, cholesterol levels, and blood cell parameters, suggesting potential influences on liver, kidney, cardiovascular, and hematological functions.
Overall, Cromoglicic acid presents as a molecule with significant acid-base properties, diverse bioactivities including antiviral, antiparasitic, enzymatic inhibition, and receptor agonism, and some potential for liver-related side effects..
Note: Summary generated by AI. Data source: ChEMBL 