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Assay Detail

CHEMBL3584692

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

Binding
Displacement of [3H]Way100635 from human recombinant 5-HT1A receptor expressed in CHO cell membranes by radioligand binding assay
17
Total Activities
17
Compounds Tested
1
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 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.
Madapa S, Harding WW.
J Nat Prod (2015) 78 : 722 -729
PubMed 25695425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.79 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56 8-OH-DPAT 1 9.15
CHEMBL3581255 1 7.04
CHEMBL3581256 1 6.99
CHEMBL3581250 1 6.93
CHEMBL3581251 1 6.82
CHEMBL3581245 1 6.82
CHEMBL3581253 1 6.79
CHEMBL228082 GLAUCINE 1 6.77
CHEMBL3580670 1 6.75
CHEMBL3581252 1 6.65
CHEMBL3581249 1 6.61
CHEMBL3581246 1 6.56
CHEMBL464099 1 6.50
CHEMBL3581254 1 6.44
CHEMBL3581244 1 6.30
CHEMBL3581248 1 6.25
CHEMBL3581247 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56 8-OH-DPAT Ki = 0.71 nM 9.15
CHEMBL3581255 Ki = 92.0 nM 7.04
CHEMBL3581256 Ki = 102.0 nM 6.99
CHEMBL3581250 Ki = 117.0 nM 6.93
CHEMBL3581251 Ki = 152.0 nM 6.82
CHEMBL3581245 Ki = 153.0 nM 6.82
CHEMBL3581253 Ki = 163.0 nM 6.79
CHEMBL228082 GLAUCINE Ki = 171.0 nM 6.77
CHEMBL3580670 Ki = 179.0 nM 6.75
CHEMBL3581252 Ki = 224.0 nM 6.65
CHEMBL3581249 Ki = 244.0 nM 6.61
CHEMBL3581246 Ki = 273.0 nM 6.56
CHEMBL464099 Ki = 314.0 nM 6.50
CHEMBL3581254 Ki = 361.0 nM 6.44
CHEMBL3581244 Ki = 506.0 nM 6.30
CHEMBL3581248 Ki = 563.0 nM 6.25
CHEMBL3581247 Ki = 845.0 nM 6.07