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Assay Detail

CHEMBL945389

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Binding
Displacement of N-[3H]methylhistamine from histamine H3 receptor in rat cortex membrane
ChEMBL ↗
44
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL4124) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel H3 receptor antagonists with improved pharmacokinetic profiles.
Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Semple G, Ren A, Pereira G, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Lorea J, Grottick AJ.
Bioorg Med Chem Lett (2008) 18 : 4133 -4136
PubMed 18554904 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 44 8.41 10.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL408934 — — 2 10.17
CHEMBL472131 — — 2 9.53
CHEMBL488464 — — 2 9.46
CHEMBL488463 — — 2 9.42
CHEMBL471555 — — 2 9.15
CHEMBL472132 — — 2 9.00
CHEMBL529892 — — 2 8.57
CHEMBL520719 — — 2 8.52
CHEMBL511657 — — 2 8.42
CHEMBL487264 — — 2 8.30
CHEMBL470286 — — 2 8.22
CHEMBL487265 — — 2 8.22
CHEMBL470480 — — 2 8.15
CHEMBL511276 — — 2 7.93
CHEMBL472505 — — 2 7.92
CHEMBL512484 — — 2 7.92
CHEMBL469689 — — 2 7.89
CHEMBL470898 — — 2 7.80
CHEMBL511973 — — 2 7.77
CHEMBL511296 — — 2 7.70
CHEMBL512707 — — 2 7.68
CHEMBL469690 — — 2 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL408934 — Ki = 0.06761 nM 10.17
CHEMBL408934 — Ki = 0.07 nM 10.15
CHEMBL472131 — Ki = 0.2951 nM 9.53
CHEMBL472131 — Ki = 0.3 nM 9.52
CHEMBL488464 — Ki = 0.3467 nM 9.46
CHEMBL488463 — Ki = 0.3802 nM 9.42
CHEMBL488463 — Ki = 0.4 nM 9.40
CHEMBL488464 — Ki = 0.4 nM 9.40
CHEMBL471555 — Ki = 0.7 nM 9.15
CHEMBL471555 — Ki = 0.7413 nM 9.13
CHEMBL472132 — Ki = 1.0 nM 9.00
CHEMBL472132 — Ki = 1.072 nM 8.97
CHEMBL529892 — Ki = 2.692 nM 8.57
CHEMBL520719 — Ki = 3.0 nM 8.52
CHEMBL529892 — Ki = 3.0 nM 8.52
CHEMBL520719 — Ki = 3.236 nM 8.49
CHEMBL511657 — Ki = 3.802 nM 8.42
CHEMBL511657 — Ki = 4.0 nM 8.40
CHEMBL487264 — Ki = 5.0 nM 8.30
CHEMBL487264 — Ki = 5.495 nM 8.26
CHEMBL487265 — Ki = 6.0 nM 8.22
CHEMBL470286 — Ki = 6.0 nM 8.22
CHEMBL470286 — Ki = 6.166 nM 8.21
CHEMBL487265 — Ki = 6.31 nM 8.20
CHEMBL470480 — Ki = 7.0 nM 8.15
CHEMBL470480 — Ki = 7.079 nM 8.15
CHEMBL511276 — Ki = 11.75 nM 7.93
CHEMBL511276 — Ki = 12.0 nM 7.92
CHEMBL472505 — Ki = 12.0 nM 7.92
CHEMBL472505 — Ki = 12.02 nM 7.92
CHEMBL512484 — Ki = 12.0 nM 7.92
CHEMBL512484 — Ki = 12.3 nM 7.91
CHEMBL469689 — Ki = 12.88 nM 7.89
CHEMBL469689 — Ki = 13.0 nM 7.89
CHEMBL470898 — Ki = 16.0 nM 7.80
CHEMBL470898 — Ki = 16.6 nM 7.78
CHEMBL511973 — Ki = 17.0 nM 7.77
CHEMBL511973 — Ki = 16.98 nM 7.77
CHEMBL511296 — Ki = 20.0 nM 7.70
CHEMBL511296 — Ki = 20.42 nM 7.69
CHEMBL512707 — Ki = 21.0 nM 7.68
CHEMBL512707 — Ki = 21.38 nM 7.67
CHEMBL469690 — Ki = 27.0 nM 7.57
CHEMBL469690 — Ki = 27.54 nM 7.56