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25CN-NBOH

Agonist of HTR2A, HTR2C, HTR2B

Structure

Information

  • HTR2A
  • HTR2C
  • HTR2B
  • Agonist
  • up to 500 nM

In Vitro Validations

Uniprot ID: P28223
Target Class: GPCR
Target SubClass: Serotonin Receptor
Potency: Ki
Potency Value: 0.81 nM
Potency Assay: Radioligand competition binding assay performed using: [3H]LSD (data shown), [3H]Cimbi-36, ([3H]ketanserin), ([3H]mesulergine)
PDB ID for probe-target interaction (3D structure): 6WHA
Target aliases:
5-hydroxytryptamine receptor 2A, HTR2, HTR2A, 5HT2 ...

DOI Reference: 10.1021/cn400216u

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Broad profiling screens performed at Eurofins and PDSP
Probe Selectivity in Vitro:
25CN-NBOH also displayed appreciable binding affinity at 5-HT6 (Ki value of 310 nM), dopamine D4 (Ki value 2.9 μM), α2A, α2B, and α2C adrenergic (Ki values of 1.2–2.9 μM), H1 histamine (Ki value of 2.1 μM), κ opioid (Ki value of 4.2 μM), and sigma-1 and -2 (Ki values of 120–280 nM) receptors
Probe Selectivity in Vitro:
Tested at a wide range of kinases and other enzymes in enzymatic assays, displaying no significant activity at 10 μM. In addition, 25CN-NBOH inhibited hERG with an IC50 value of 2.7 µM.
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SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Need to be aware compound is active on multiple targets - HTR2A, HTR2B, and HTR2C - when drawing biological conclusions from studies carried out with this compound.
Important to measure drug concentrations in any efficacy studies to put other pharmacology into context:  sigma-1 (Ki = 284 nM), α2C (Ki = 543 nM), 5-HT6 (Ki = 573 nM), sigma-2 (Ki = 575 nM), α2A (Ki = 803 nM)

(last updated: 25 Jul 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 4 Aug 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Mode of in vivo delivery i.p or s.c. @ 1.5 mg/kg is indicated by Buchborn 2018.  Note potential for rapid desensitization in mouse models

(last updated: 13 Aug 2020 )