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Assay Detail

CHEMBL930591

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

Binding
Displacement of N-[3H]methylhistamine from histamine H3 receptor in rat cortex
ChEMBL ↗
49
Total Activities
25
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

A new family of H3 receptor antagonists based on the natural product Conessine.
Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Sengupta D, Duffield JJ, Semple G, Webb RR, Sage C, Ren A, Pereira G, Knudsen J, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Whelan K, Grottick AJ.
Bioorg Med Chem Lett (2008) 18 : 1490 -1494
PubMed 18194865 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 49 8.82 10.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL270011 — — 2 10.35
CHEMBL255962 — — 2 10.30
CHEMBL408934 — — 2 10.17
CHEMBL401954 — — 2 10.11
CHEMBL402640 — — 2 10.00
CHEMBL402297 — — 2 9.80
CHEMBL255840 — — 2 9.54
CHEMBL255752 — — 2 9.52
CHEMBL256225 — — 2 9.43
CHEMBL410623 — — 2 9.40
CHEMBL255961 — — 2 9.29
CHEMBL409899 — — 2 9.12
CHEMBL270440 — — 2 9.05
CHEMBL255166 — — 2 8.77
CHEMBL429418 — — 2 8.70
CHEMBL273202 — — 2 8.64
CHEMBL256648 — — 2 8.62
CHEMBL402296 — — 2 8.56
CHEMBL258302 — — 2 8.17
CHEMBL255847 — — 2 7.45
CHEMBL404753 — — 2 7.24
CHEMBL191703 CONESSINE 2.0 1 7.18
CHEMBL270439 — — 2 7.17
CHEMBL270241 — — 2 6.88
CHEMBL437404 — — 2 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL270011 — Ki = 0.04467 nM 10.35
CHEMBL270011 — Ki = 0.05 nM 10.30
CHEMBL255962 — Ki = 0.05 nM 10.30
CHEMBL255962 — Ki = 0.05888 nM 10.23
CHEMBL408934 — Ki = 0.06761 nM 10.17
CHEMBL408934 — Ki = 0.07 nM 10.15
CHEMBL401954 — Ki = 0.07762 nM 10.11
CHEMBL401954 — Ki = 0.08 nM 10.10
CHEMBL402640 — Ki = 0.1 nM 10.00
CHEMBL402640 — Ki = 0.1122 nM 9.95
CHEMBL402297 — Ki = 0.16 nM 9.80
CHEMBL402297 — Ki = 0.1585 nM 9.80
CHEMBL255840 — Ki = 0.29 nM 9.54
CHEMBL255840 — Ki = 0.2951 nM 9.53
CHEMBL255752 — Ki = 0.3 nM 9.52
CHEMBL255752 — Ki = 0.309 nM 9.51
CHEMBL256225 — Ki = 0.3715 nM 9.43
CHEMBL410623 — Ki = 0.4 nM 9.40
CHEMBL256225 — Ki = 0.4 nM 9.40
CHEMBL410623 — Ki = 0.4169 nM 9.38
CHEMBL255961 — Ki = 0.5129 nM 9.29
CHEMBL255961 — Ki = 0.51 nM 9.29
CHEMBL409899 — Ki = 0.7586 nM 9.12
CHEMBL409899 — Ki = 0.75 nM 9.12
CHEMBL270440 — Ki = 0.9 nM 9.05
CHEMBL270440 — Ki = 0.955 nM 9.02
CHEMBL255166 — Ki = 1.698 nM 8.77
CHEMBL255166 — Ki = 1.7 nM 8.77
CHEMBL429418 — Ki = 2.0 nM 8.70
CHEMBL273202 — Ki = 2.291 nM 8.64
CHEMBL273202 — Ki = 2.3 nM 8.64
CHEMBL429418 — Ki = 2.344 nM 8.63
CHEMBL256648 — Ki = 2.4 nM 8.62
CHEMBL256648 — Ki = 2.399 nM 8.62
CHEMBL402296 — Ki = 2.754 nM 8.56
CHEMBL402296 — Ki = 2.8 nM 8.55
CHEMBL258302 — Ki = 6.761 nM 8.17
CHEMBL258302 — Ki = 7.0 nM 8.15
CHEMBL255847 — Ki = 35.48 nM 7.45
CHEMBL255847 — Ki = 36.0 nM 7.44
CHEMBL404753 — Ki = 58.0 nM 7.24
CHEMBL404753 — Ki = 58.88 nM 7.23
CHEMBL191703 CONESSINE Ki = 66.0 nM 7.18
CHEMBL270439 — Ki = 67.61 nM 7.17
CHEMBL270439 — Ki = 67.0 nM 7.17
CHEMBL270241 — Ki = 131.83 nM 6.88
CHEMBL437404 — Ki = 257.04 nM 6.59
CHEMBL437404 — Ki = 256.0 nM 6.59
CHEMBL270241 — Ki = 310.0 nM 6.51