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Assay Detail

CHEMBL866473

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

Binding
Displacement of [3H]N-alpha-methylhistamine from guinea pig histamine H3 receptor
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Histamine H3 receptor (CHEMBL5076)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists.
Berlin M, Ting PC, Vaccaro WD, Aslanian R, McCormick KD, Lee JF, Albanese MM, Mutahi MW, Piwinski JJ, Shih NY, Duguma L, Solomon DM, Zhou W, Sher R, Favreau L, Bryant M, Korfmacher WA, Nardo C, West RE, Anthes JC, Williams SM, Wu RL, Susan She H, Rivelli MA, Corboz MR, Hey JA.
Bioorg Med Chem Lett (2006) 16 : 989 -994
PubMed 16297617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 7.91 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL380525 1 9.00
CHEMBL381741 1 8.52
CHEMBL380139 1 8.52
CHEMBL205129 1 8.52
CHEMBL424675 1 8.52
CHEMBL200267 1 8.40
CHEMBL379445 1 8.40
CHEMBL203696 1 8.40
CHEMBL377500 1 8.40
CHEMBL204193 1 8.30
CHEMBL204606 1 8.22
CHEMBL378821 1 8.10
CHEMBL204639 1 8.05
CHEMBL204235 1 8.00
CHEMBL382677 1 7.92
CHEMBL437500 1 7.92
CHEMBL203983 1 7.92
CHEMBL439689 1 7.89
CHEMBL204951 1 7.82
CHEMBL379885 1 7.82
CHEMBL204301 1 7.80
CHEMBL203604 1 7.80
CHEMBL203910 1 7.77
CHEMBL425765 1 7.64
CHEMBL204742 1 7.62
CHEMBL203805 1 7.58
CHEMBL381717 1 7.48
CHEMBL204705 1 7.47
CHEMBL426487 1 7.40
CHEMBL204640 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL380525 Ki = 1.0 nM 9.00
CHEMBL381741 Ki = 3.0 nM 8.52
CHEMBL424675 Ki = 3.0 nM 8.52
CHEMBL205129 Ki = 3.0 nM 8.52
CHEMBL380139 Ki = 3.0 nM 8.52
CHEMBL200267 Ki = 4.0 nM 8.40
CHEMBL379445 Ki = 4.0 nM 8.40
CHEMBL203696 Ki = 4.0 nM 8.40
CHEMBL377500 Ki = 4.0 nM 8.40
CHEMBL204193 Ki = 5.0 nM 8.30
CHEMBL204606 Ki = 6.0 nM 8.22
CHEMBL378821 Ki = 8.0 nM 8.10
CHEMBL204639 Ki = 9.0 nM 8.05
CHEMBL204235 Ki = 10.0 nM 8.00
CHEMBL203983 Ki = 12.0 nM 7.92
CHEMBL382677 Ki = 12.0 nM 7.92
CHEMBL437500 Ki = 12.0 nM 7.92
CHEMBL439689 Ki = 13.0 nM 7.89
CHEMBL204951 Ki = 15.0 nM 7.82
CHEMBL379885 Ki = 15.0 nM 7.82
CHEMBL204301 Ki = 16.0 nM 7.80
CHEMBL203604 Ki = 16.0 nM 7.80
CHEMBL203910 Ki = 17.0 nM 7.77
CHEMBL425765 Ki = 23.0 nM 7.64
CHEMBL204742 Ki = 24.0 nM 7.62
CHEMBL203805 Ki = 26.0 nM 7.58
CHEMBL381717 Ki = 33.0 nM 7.48
CHEMBL204705 Ki = 34.0 nM 7.47
CHEMBL426487 Ki = 40.0 nM 7.40
CHEMBL204640 Ki = 45.0 nM 7.35
CHEMBL381070 Ki = 45.0 nM 7.35
CHEMBL377278 Ki = 51.0 nM 7.29
CHEMBL204587 Ki = 52.0 nM 7.28
CHEMBL203912 Ki = 315.0 nM 6.50