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Assay Detail

CHEMBL833493

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

Binding
Displacement of [3H]8-hydroxy-2-(di-n-propylamino)tetralin from human 5-hydroxytryptamine 1A receptor
11
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.
Bolognesi ML, Budriesi R, Cavalli A, Chiarini A, Gotti R, Leonardi A, Minarini A, Poggesi E, Recanatini M, Rosini M, Tumiatti V, Melchiorre C.
J Med Chem (1999) 42 : 4214 -4224
PubMed 10514291 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.14 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135974 1 9.08
CHEMBL13647 BMY-7378 1 9.03
CHEMBL25554 1 8.68
CHEMBL56 8-OH-DPAT 1 8.46
CHEMBL132378 1 8.43
CHEMBL135973 1 8.26
CHEMBL134428 1 7.65
CHEMBL2112711 2 7.61
CHEMBL2112713 2 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135974 Ki = 0.8318 nM 9.08
CHEMBL13647 BMY-7378 Ki = 0.9333 nM 9.03
CHEMBL25554 Ki = 2.089 nM 8.68
CHEMBL56 8-OH-DPAT Ki = 3.467 nM 8.46
CHEMBL132378 Ki = 3.715 nM 8.43
CHEMBL135973 Ki = 5.495 nM 8.26
CHEMBL134428 Ki = 22.39 nM 7.65
CHEMBL2112711 Ki = 24.55 nM 7.61
CHEMBL2112711 Ki = 26.92 nM 7.57
CHEMBL2112713 Ki = 33.88 nM 7.47
CHEMBL2112713 Ki = 50.12 nM 7.30