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Assay Detail

CHEMBL693109

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Binding
Binding affinity for human histamine H3 receptor
39
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel human histamine H(3) receptor antagonists.
Shah C, McAtee L, Breitenbucher JG, Rudolph D, Li X, Lovenberg TW, Mazur C, Wilson SJ, Carruthers NI.
Bioorg Med Chem Lett (2002) 12 : 3309 -3312
PubMed 12392739 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 6.66 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49532 1 8.70
CHEMBL112621 1 8.70
CHEMBL72022 2 8.52
CHEMBL324650 1 8.30
CHEMBL112011 1 8.22
CHEMBL48982 1 8.22
CHEMBL111930 1 8.15
CHEMBL113551 1 8.00
CHEMBL70944 1 7.89
CHEMBL113236 1 7.82
CHEMBL110015 1 7.77
CHEMBL326718 1 7.66
CHEMBL431083 1 7.55
CHEMBL306911 1 7.37
CHEMBL112912 1 7.16
CHEMBL70756 1 7.10
CHEMBL114231 1 6.52
CHEMBL325465 1 6.30
CHEMBL445619 1 6.06
CHEMBL421680 1 6.00
CHEMBL71248 1 5.96
CHEMBL71352 1 5.89
CHEMBL70383 1 5.82
CHEMBL71693 1 5.77
CHEMBL310907 1 5.72
CHEMBL113145 1 5.70
CHEMBL70313 1 5.68
CHEMBL302591 1 5.62
CHEMBL308142 1 5.57
CHEMBL70946 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49532 Ki = 2.0 nM 8.70
CHEMBL112621 Ki = 2.0 nM 8.70
CHEMBL72022 Ki = 3.0 nM 8.52
CHEMBL72022 Ki = 3.0 nM 8.52
CHEMBL324650 Ki = 5.0 nM 8.30
CHEMBL112011 Ki = 6.0 nM 8.22
CHEMBL48982 Ki = 6.0 nM 8.22
CHEMBL111930 Ki = 7.0 nM 8.15
CHEMBL113551 Ki = 10.0 nM 8.00
CHEMBL70944 Ki = 13.0 nM 7.89
CHEMBL113236 Ki = 15.0 nM 7.82
CHEMBL110015 Ki = 17.0 nM 7.77
CHEMBL326718 Ki = 22.0 nM 7.66
CHEMBL431083 Ki = 28.0 nM 7.55
CHEMBL306911 Ki = 43.0 nM 7.37
CHEMBL112912 Ki = 69.0 nM 7.16
CHEMBL70756 Ki = 80.0 nM 7.10
CHEMBL114231 Ki = 300.0 nM 6.52
CHEMBL325465 Ki = 500.0 nM 6.30
CHEMBL445619 Ki = 870.0 nM 6.06
CHEMBL421680 Ki = 1000.0 nM 6.00
CHEMBL71248 Ki = 1100.0 nM 5.96
CHEMBL71352 Ki = 1300.0 nM 5.89
CHEMBL70383 Ki = 1500.0 nM 5.82
CHEMBL71693 Ki = 1700.0 nM 5.77
CHEMBL310907 Ki = 1900.0 nM 5.72
CHEMBL113145 Ki = 2000.0 nM 5.70
CHEMBL70313 Ki = 2100.0 nM 5.68
CHEMBL302591 Ki = 2400.0 nM 5.62
CHEMBL308142 Ki = 2700.0 nM 5.57
CHEMBL70946 Ki = 2900.0 nM 5.54
CHEMBL71530 Ki = 3300.0 nM 5.48
CHEMBL112163 Ki = 4000.0 nM 5.40
CHEMBL70874 Ki = 4200.0 nM 5.38
CHEMBL114470 Ki = 4800.0 nM 5.32
CHEMBL112647 Ki = 5400.0 nM 5.27
CHEMBL70945 Ki = 7900.0 nM 5.10
CHEMBL71476 Ki = 8000.0 nM 5.10
CHEMBL71047 Ki = 11000.0 nM 4.96