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Assay Detail

CHEMBL838601

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Binding
Mean functional activity against human H3 receptor
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

4-phenoxypiperidines: potent, conformationally restricted, non-imidazole histamine H3 antagonists.
Dvorak CA, Apodaca R, Barbier AJ, Berridge CW, Wilson SJ, Boggs JD, Xiao W, Lovenberg TW, Carruthers NI.
J Med Chem (2005) 48 : 2229 -2238
PubMed 15771465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 21 9.25 9.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL194441 1 9.90
CHEMBL129542 JNJ-5207852 1 9.84
CHEMBL427177 1 9.76
CHEMBL193381 1 9.67
CHEMBL372471 1 9.59
CHEMBL194541 1 9.59
CHEMBL195815 1 9.49
CHEMBL193934 1 9.48
CHEMBL439676 1 9.47
CHEMBL370169 1 9.45
CHEMBL195826 1 9.34
CHEMBL191405 1 9.33
CHEMBL194092 1 9.32
CHEMBL194090 1 9.18
CHEMBL372935 1 9.13
CHEMBL195099 1 9.09
CHEMBL193861 1 8.99
CHEMBL191992 1 8.93
CHEMBL195777 1 8.69
CHEMBL194548 1 8.57
CHEMBL260374 THIOPERAMIDE 1 7.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL194441 Kd = 0.1259 nM 9.90
CHEMBL129542 JNJ-5207852 Kd = 0.1445 nM 9.84
CHEMBL427177 Kd = 0.1738 nM 9.76
CHEMBL193381 Kd = 0.2138 nM 9.67
CHEMBL372471 Kd = 0.257 nM 9.59
CHEMBL194541 Kd = 0.257 nM 9.59
CHEMBL195815 Kd = 0.3236 nM 9.49
CHEMBL193934 Kd = 0.3311 nM 9.48
CHEMBL439676 Kd = 0.3388 nM 9.47
CHEMBL370169 Kd = 0.3548 nM 9.45
CHEMBL195826 Kd = 0.4571 nM 9.34
CHEMBL191405 Kd = 0.4677 nM 9.33
CHEMBL194092 Kd = 0.4786 nM 9.32
CHEMBL194090 Kd = 0.6607 nM 9.18
CHEMBL372935 Kd = 0.7413 nM 9.13
CHEMBL195099 Kd = 0.8128 nM 9.09
CHEMBL193861 Kd = 1.023 nM 8.99
CHEMBL191992 Kd = 1.175 nM 8.93
CHEMBL195777 Kd = 2.042 nM 8.69
CHEMBL194548 Kd = 2.692 nM 8.57
CHEMBL260374 THIOPERAMIDE Kd = 43.65 nM 7.36