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Assay Detail

CHEMBL617062

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

Binding
Ability to displace [125I]R91150 from human cloned 5-hydroxytryptamine 2A receptor expressed in L929 cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type L929
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of 2-(aminoalkyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives: a novel series of 5-HT(2A/2C) receptor antagonists.
Cid J, Alonso JM, Andrés JI, Fernández J, Gil P, Iturrino L, Matesanz E, Meert TF, Megens A, Sipido VK, Trabanco AA.
Bioorg Med Chem Lett (2004) 14 : 2765 -2771
PubMed 15125929 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.15 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL328573 1 8.60
CHEMBL329566 1 8.60
CHEMBL316068 1 7.76
CHEMBL329268 1 7.71
CHEMBL92667 1 7.66
CHEMBL327306 1 7.51
CHEMBL96158 1 7.43
CHEMBL329685 1 7.31
CHEMBL92333 1 7.25
CHEMBL314968 1 7.16
CHEMBL2112371 1 7.13
CHEMBL328356 1 7.09
CHEMBL92337 1 7.06
CHEMBL93321 1 7.04
CHEMBL330713 1 7.03
CHEMBL96732 1 6.99
CHEMBL327651 1 6.98
CHEMBL318659 1 6.36
CHEMBL328662 1 6.36
CHEMBL96429 1 6.36
CHEMBL328209 1 5.97
CHEMBL96471 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL328573 Ki = 2.5 nM 8.60
CHEMBL329566 Ki = 2.5 nM 8.60
CHEMBL316068 Ki = 17.3 nM 7.76
CHEMBL329268 Ki = 19.6 nM 7.71
CHEMBL92667 Ki = 21.7 nM 7.66
CHEMBL327306 Ki = 30.7 nM 7.51
CHEMBL96158 Ki = 37.0 nM 7.43
CHEMBL329685 Ki = 48.6 nM 7.31
CHEMBL92333 Ki = 56.0 nM 7.25
CHEMBL314968 Ki = 68.7 nM 7.16
CHEMBL2112371 Ki = 74.1 nM 7.13
CHEMBL328356 Ki = 80.7 nM 7.09
CHEMBL92337 Ki = 86.5 nM 7.06
CHEMBL93321 Ki = 90.5 nM 7.04
CHEMBL330713 Ki = 92.6 nM 7.03
CHEMBL96732 Ki = 102.0 nM 6.99
CHEMBL327651 Ki = 104.0 nM 6.98
CHEMBL318659 Ki = 433.0 nM 6.36
CHEMBL328662 Ki = 433.0 nM 6.36
CHEMBL96429 Ki = 433.0 nM 6.36
CHEMBL328209 Ki = 1064.0 nM 5.97
CHEMBL96471 Ki = 1088.0 nM 5.96