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Assay Detail

CHEMBL3820063

Review assay metadata, readout intent, target linkage, and publication context from the same page.

ADMET
Displacement of [3H]LSD from human recombinant 5HT2B receptor incubated for 1.5 hrs by microbeta scintillation counting method
18
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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

Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.
Etukala JR, Zhu XY, Eyunni SV, Onyameh EK, Ofori E, Bricker BA, Kang HJ, Huang XP, Roth BL, Ablordeppey SY.
Bioorg Med Chem (2016) 24 : 3671 -3679
PubMed 27364609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.56 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3818124 2 7.44
CHEMBL3818805 2 7.29
CHEMBL3819567 2 6.91
CHEMBL3818478 2 6.70
CHEMBL3819434 2 6.47
CHEMBL3819153 2 6.29
CHEMBL3818881 2 6.12
CHEMBL3818935 2 6.04
CHEMBL2037526 2 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3818124 Ki = 36.31 nM 7.44
CHEMBL3818124 Ki = 36.0 nM 7.44
CHEMBL3818805 Ki = 51.29 nM 7.29
CHEMBL3818805 Ki = 51.0 nM 7.29
CHEMBL3819567 Ki = 123.03 nM 6.91
CHEMBL3819567 Ki = 122.0 nM 6.91
CHEMBL3818478 Ki = 202.0 nM 6.70
CHEMBL3818478 Ki = 204.17 nM 6.69
CHEMBL3819434 Ki = 338.84 nM 6.47
CHEMBL3819434 Ki = 342.0 nM 6.47
CHEMBL3819153 Ki = 515.0 nM 6.29
CHEMBL3819153 Ki = 512.86 nM 6.29
CHEMBL3818881 Ki = 758.0 nM 6.12
CHEMBL3818881 Ki = 758.58 nM 6.12
CHEMBL3818935 Ki = 905.0 nM 6.04
CHEMBL3818935 Ki = 912.01 nM 6.04
CHEMBL2037526 Ki = 1584.89 nM 5.80
CHEMBL2037526 Ki = 1578.0 nM 5.80