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Assay Detail

CHEMBL617894

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

Binding
Ability to displace [3H]- mesulergine from human cloned 5-hydroxytryptamine 2C receptor expressed in CHO cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
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 7.51 9.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL329566 1 9.03
CHEMBL328573 1 9.00
CHEMBL329268 1 8.49
CHEMBL92667 1 8.17
CHEMBL329685 1 8.01
CHEMBL328356 1 7.89
CHEMBL2112371 1 7.80
CHEMBL328662 1 7.77
CHEMBL327306 1 7.61
CHEMBL96429 1 7.57
CHEMBL327651 1 7.55
CHEMBL96158 1 7.51
CHEMBL93321 1 7.49
CHEMBL96471 1 7.37
CHEMBL92333 1 6.97
CHEMBL316068 1 6.92
CHEMBL328209 1 6.91
CHEMBL96732 1 6.78
CHEMBL92337 1 6.77
CHEMBL330713 1 6.74
CHEMBL314968 1 6.62
CHEMBL318659 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL329566 Ki = 0.93 nM 9.03
CHEMBL328573 Ki = 1.0 nM 9.00
CHEMBL329268 Ki = 3.25 nM 8.49
CHEMBL92667 Ki = 6.7 nM 8.17
CHEMBL329685 Ki = 9.7 nM 8.01
CHEMBL328356 Ki = 12.9 nM 7.89
CHEMBL2112371 Ki = 15.9 nM 7.80
CHEMBL328662 Ki = 17.0 nM 7.77
CHEMBL327306 Ki = 24.7 nM 7.61
CHEMBL96429 Ki = 27.0 nM 7.57
CHEMBL327651 Ki = 28.0 nM 7.55
CHEMBL96158 Ki = 31.0 nM 7.51
CHEMBL93321 Ki = 32.5 nM 7.49
CHEMBL96471 Ki = 42.7 nM 7.37
CHEMBL92333 Ki = 107.4 nM 6.97
CHEMBL316068 Ki = 120.0 nM 6.92
CHEMBL328209 Ki = 123.5 nM 6.91
CHEMBL96732 Ki = 166.0 nM 6.78
CHEMBL92337 Ki = 170.0 nM 6.77
CHEMBL330713 Ki = 183.0 nM 6.74
CHEMBL314968 Ki = 239.0 nM 6.62
CHEMBL318659 Ki = 677.0 nM 6.17