Assay Detail

CHEMBL5161220

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Toxicity

Inhibition of 5HT2B receptor (unknown origin)

ChEMBL ↗

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Target

5-hydroxytryptamine receptor 2B (CHEMBL1833) ↗

Open DB target context

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5-hydroxytryptamine receptor 2B (CHEMBL1833) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target 5-hydroxytryptamine receptor 2B

CHEMBL1833

Anchored from Assay target.

Protein identity 5-hydroxytryptamine receptor 2B

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Toxicity
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

5-hydroxytryptamine receptor 2B (CHEMBL1833) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.

Luo G, Chen L, Kostich WA, Hamman B, Allen J, Easton A, Bourin C, Gulianello M, Lippy J, Nara S, Pattipati SN, Dandapani K, Dokania M, Vattikundala P, Sharma V, Elavazhagan S, Verma MK, Lal Das M, Wagh S, Balakrishnan A, Johnson BM, Santone KS, Thalody G, Denton R, Saminathan H, Holenarsipur VK, Kumar A, Rao A, Putlur SP, Sarvasiddhi SK, Shankar G, Louis JV, Ramarao M, Conway CM, Li YW, Pieschl R, Tian Y, Hong Y, Bristow L, Albright CF, Bronson JJ, Macor JE, Dzierba CD.
J Med Chem (2022) 65 : 4534 -4564
PubMed 35261239 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	6.27	6.27

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5170576	—	—	1	6.27

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5170576	—	IC50	=	540.0	nM	6.27