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Assay Detail

CHEMBL5054014

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

Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
7
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2B (CHEMBL1833)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Activity of <i>Mitragyna speciosa</i> ("Kratom") Alkaloids at Serotonin Receptors.
León F, Obeng S, Mottinelli M, Chen Y, King TI, Berthold EC, Kamble SH, Restrepo LF, Patel A, Gamez-Jimenez LR, Lopera-Londoño C, Hiranita T, Sharma A, Hampson AJ, Canal CE, McMahon LR, McCurdy CR.
J Med Chem (2021) 64 : 13510 -13523
PubMed 34467758 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.00 8.66
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134519 1 8.66
CHEMBL4848517 1 7.70
CHEMBL4859858 1 7.64
CHEMBL8412 IPSAPIRONE 2.0 1 -
CHEMBL56 8-OH-DPAT 1 -
CHEMBL31354 WAY-100,635 1 -
CHEMBL297784 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134519 Ki = 2.2 nM 8.66
CHEMBL4848517 Ki = 20.0 nM 7.70
CHEMBL4859858 Ki = 23.0 nM 7.64
CHEMBL8412 IPSAPIRONE Ki - -
CHEMBL56 8-OH-DPAT Ki - -
CHEMBL31354 WAY-100,635 Ki - -
CHEMBL297784 Activity - -