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Assay Detail

CHEMBL5054018

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

Binding
Displacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assay
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 7 (CHEMBL3155)
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 6.39 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 1 8.68
CHEMBL4848517 1 6.06
CHEMBL4859858 1 5.80
CHEMBL299031 1 5.00
CHEMBL5072247 1 -
CHEMBL5089613 1 -
CHEMBL8412 IPSAPIRONE 2.0 1 -
CHEMBL56 8-OH-DPAT 1 -
CHEMBL134519 1 -
CHEMBL31354 WAY-100,635 1 -
CHEMBL297784 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN Ki = 2.1 nM 8.68
CHEMBL4848517 Ki = 870.0 nM 6.06
CHEMBL4859858 Ki = 1600.0 nM 5.80
CHEMBL299031 Ki = 10000.0 nM 5.00
CHEMBL5072247 Ki - -
CHEMBL5089613 Ki - -
CHEMBL8412 IPSAPIRONE Ki - -
CHEMBL56 8-OH-DPAT Ki - -
CHEMBL134519 Ki - -
CHEMBL31354 WAY-100,635 Ki - -
CHEMBL297784 Ki - -