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Assay Detail

CHEMBL691453

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

Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 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

Histamine H1 receptor (CHEMBL231)
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 8.24 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL329566 1 9.27
CHEMBL329268 1 9.20
CHEMBL328573 1 9.19
CHEMBL92667 1 9.15
CHEMBL316068 1 8.92
CHEMBL328662 1 8.72
CHEMBL96429 1 8.63
CHEMBL318659 1 8.52
CHEMBL2112371 1 8.46
CHEMBL327651 1 8.43
CHEMBL92337 1 8.43
CHEMBL327306 1 8.37
CHEMBL328356 1 8.22
CHEMBL329685 1 8.03
CHEMBL93321 1 8.02
CHEMBL96158 1 7.85
CHEMBL328209 1 7.69
CHEMBL96732 1 7.57
CHEMBL96471 1 7.53
CHEMBL330713 1 7.49
CHEMBL314968 1 7.33
CHEMBL92333 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL329566 Ki = 0.54 nM 9.27
CHEMBL329268 Ki = 0.63 nM 9.20
CHEMBL328573 Ki = 0.64 nM 9.19
CHEMBL92667 Ki = 0.7 nM 9.15
CHEMBL316068 Ki = 1.2 nM 8.92
CHEMBL328662 Ki = 1.9 nM 8.72
CHEMBL96429 Ki = 2.36 nM 8.63
CHEMBL318659 Ki = 3.0 nM 8.52
CHEMBL2112371 Ki = 3.5 nM 8.46
CHEMBL327651 Ki = 3.74 nM 8.43
CHEMBL92337 Ki = 3.7 nM 8.43
CHEMBL327306 Ki = 4.3 nM 8.37
CHEMBL328356 Ki = 6.0 nM 8.22
CHEMBL329685 Ki = 9.3 nM 8.03
CHEMBL93321 Ki = 9.6 nM 8.02
CHEMBL96158 Ki = 14.0 nM 7.85
CHEMBL328209 Ki = 20.6 nM 7.69
CHEMBL96732 Ki = 27.0 nM 7.57
CHEMBL96471 Ki = 29.7 nM 7.53
CHEMBL330713 Ki = 32.6 nM 7.49
CHEMBL314968 Ki = 47.1 nM 7.33
CHEMBL92333 Ki = 471.0 nM 6.33