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Assay Detail

CHEMBL5054017

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

Binding
Displacement of [3H]LSD from human recombinant 5-HT2A receptor expressed in HEK cells by radioligand completion assay relative to control
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
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 11 6.64 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134519 1 8.17
CHEMBL39 SEROTONIN 3.0 1 7.76
CHEMBL4848517 1 6.09
CHEMBL4859858 1 5.88
CHEMBL299031 1 5.30
CHEMBL5072247 1 -
CHEMBL5089613 1 -
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 = 6.8 nM 8.17
CHEMBL39 SEROTONIN Ki = 17.2 nM 7.76
CHEMBL4848517 Ki = 815.0 nM 6.09
CHEMBL4859858 Ki = 1320.0 nM 5.88
CHEMBL299031 Ki = 5010.0 nM 5.30
CHEMBL5072247 Ki - -
CHEMBL5089613 Ki - -
CHEMBL8412 IPSAPIRONE Ki - -
CHEMBL56 8-OH-DPAT Ki - -
CHEMBL31354 WAY-100,635 Ki - -
CHEMBL297784 Ki - -