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Assay Detail

CHEMBL972067

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

Binding
Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells
13
Total Activities
7
Compounds Tested
3
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

Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.
Gafner S, Dietz BM, McPhail KL, Scott IM, Glinski JA, Russell FE, McCollom MM, Budzinski JW, Foster BC, Bergeron C, Rhyu MR, Bolton JL.
J Nat Prod (2006) 69 : 432 -435
PubMed 16562853 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.23 8.12
Activity 4 - -
Ki 2 6.15 7.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19215 METERGOLINE 2.0 1 8.12
CHEMBL464099 2 7.07
CHEMBL481839 ESCHOLTZINE 2 5.22
CHEMBL480663 CARYACHINE 2 5.05
CHEMBL538357 CALIFORNIDINE 2 -
CHEMBL50 QUERCETIN 3.0 2 -
CHEMBL486179 PROTOPINE 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19215 METERGOLINE EC50 = 7.5 nM 8.12
CHEMBL464099 Ki = 85.0 nM 7.07
CHEMBL464099 EC50 = 160.0 nM 6.80
CHEMBL481839 ESCHOLTZINE Ki = 6000.0 nM 5.22
CHEMBL480663 CARYACHINE EC50 = 9000.0 nM 5.05
CHEMBL481839 ESCHOLTZINE EC50 = 11000.0 nM 4.96
CHEMBL538357 CALIFORNIDINE EC50 > 100000.0 nM -
CHEMBL538357 CALIFORNIDINE Activity - -
CHEMBL50 QUERCETIN EC50 > 100000.0 nM -
CHEMBL50 QUERCETIN Activity - -
CHEMBL486179 PROTOPINE EC50 > 100000.0 nM -
CHEMBL486179 PROTOPINE Activity - -
CHEMBL480663 CARYACHINE Activity = 5.0 uM -