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Assay Detail

CHEMBL897804

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Binding
Binding affinity to human histamine H3 receptor
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H3 receptor (CHEMBL264)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors.
Letavic MA, Stocking EM, Barbier AJ, Bonaventure P, Boggs JD, Lord B, Miller KL, Wilson SJ, Carruthers NI.
Bioorg Med Chem Lett (2007) 17 : 4799 -4803
PubMed 17616397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 7.82 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129542 JNJ-5207852 1 9.22
CHEMBL235614 1 9.15
CHEMBL237087 1 8.89
CHEMBL393036 1 8.77
CHEMBL194092 1 8.68
CHEMBL397575 1 8.52
CHEMBL236674 1 8.52
CHEMBL235824 1 8.40
CHEMBL238143 1 8.33
CHEMBL238141 1 8.28
CHEMBL237317 1 8.27
CHEMBL428024 1 8.24
CHEMBL391074 1 8.22
CHEMBL397577 1 8.22
CHEMBL237512 1 8.21
CHEMBL236252 1 8.15
CHEMBL236475 1 8.15
CHEMBL236675 1 8.14
CHEMBL237513 1 8.01
CHEMBL236010 1 8.01
CHEMBL391947 1 7.96
CHEMBL236047 1 7.96
CHEMBL236046 1 7.96
CHEMBL236676 1 7.89
CHEMBL237319 1 7.89
CHEMBL237747 1 7.85
CHEMBL442080 1 7.77
CHEMBL235814 1 7.77
CHEMBL441137 1 7.51
CHEMBL238182 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129542 JNJ-5207852 Ki = 0.6 nM 9.22
CHEMBL235614 Ki = 0.7 nM 9.15
CHEMBL237087 Ki = 1.3 nM 8.89
CHEMBL393036 Ki = 1.7 nM 8.77
CHEMBL194092 Ki = 2.1 nM 8.68
CHEMBL397575 Ki = 3.0 nM 8.52
CHEMBL236674 Ki = 3.0 nM 8.52
CHEMBL235824 Ki = 4.0 nM 8.40
CHEMBL238143 Ki = 4.7 nM 8.33
CHEMBL238141 Ki = 5.2 nM 8.28
CHEMBL237317 Ki = 5.4 nM 8.27
CHEMBL428024 Ki = 5.7 nM 8.24
CHEMBL391074 Ki = 6.0 nM 8.22
CHEMBL397577 Ki = 6.0 nM 8.22
CHEMBL237512 Ki = 6.1 nM 8.21
CHEMBL236252 Ki = 7.0 nM 8.15
CHEMBL236475 Ki = 7.0 nM 8.15
CHEMBL236675 Ki = 7.3 nM 8.14
CHEMBL237513 Ki = 9.7 nM 8.01
CHEMBL236010 Ki = 9.7 nM 8.01
CHEMBL391947 Ki = 11.0 nM 7.96
CHEMBL236047 Ki = 11.0 nM 7.96
CHEMBL236046 Ki = 11.0 nM 7.96
CHEMBL236676 Ki = 13.0 nM 7.89
CHEMBL237319 Ki = 13.0 nM 7.89
CHEMBL237747 Ki = 14.0 nM 7.85
CHEMBL235814 Ki = 17.0 nM 7.77
CHEMBL442080 Ki = 17.0 nM 7.77
CHEMBL441137 Ki = 31.0 nM 7.51
CHEMBL238182 Ki = 52.0 nM 7.28
CHEMBL398981 Ki = 93.0 nM 7.03
CHEMBL235794 Ki = 423.0 nM 6.37
CHEMBL237514 Ki = 864.0 nM 6.06
CHEMBL393009 Ki = 1867.0 nM 5.73
CHEMBL41 FLUOXETINE Ki = 7300.0 nM 5.14
CHEMBL237521 Ki = 9000.0 nM 5.05