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Assay Detail

CHEMBL4815472

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

Binding
Displacement of [3H]UR-P129 from human histamine H3 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL ↗
51
Total Activities
51
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H<sub>2</sub>R and D<sub>3</sub>R.
Biselli S, Bresinsky M, Tropmann K, Forster L, Honisch C, Buschauer A, Bernhardt G, Pockes S.
Eur J Med Chem (2021) 214 : 113190 -113190
PubMed 33548637 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 4.79 7.59
pKi 9 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL90 HISTAMINE 4.0 1 7.59
CHEMBL4876799 — — 1 5.82
CHEMBL4846201 — — 1 5.64
CHEMBL4853107 — — 1 5.49
CHEMBL4878215 — — 1 5.48
CHEMBL4853668 — — 1 5.25
CHEMBL4857560 — — 1 5.13
CHEMBL4871482 — — 1 5.10
CHEMBL4865765 — — 1 5.04
CHEMBL4876025 — — 1 5.04
CHEMBL4846638 — — 1 5.00
CHEMBL4866734 — — 1 5.00
CHEMBL4860528 — — 1 4.98
CHEMBL4872375 — — 1 4.96
CHEMBL4856572 — — 1 4.93
CHEMBL4876267 — — 1 4.89
CHEMBL4863523 — — 1 4.84
CHEMBL4848815 — — 1 4.78
CHEMBL4852212 — — 1 4.77
CHEMBL4863347 — — 1 4.75
CHEMBL4858849 — — 1 4.72
CHEMBL4856005 — — 1 4.71
CHEMBL4870510 — — 1 4.66
CHEMBL4848697 — — 1 4.59
CHEMBL4869194 — — 1 4.58
CHEMBL4869389 — — 1 4.57
CHEMBL4864852 — — 1 4.51
CHEMBL4850448 — — 1 4.50
CHEMBL4867962 — — 1 4.48
CHEMBL4848026 — — 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL90 HISTAMINE Ki = 25.7 nM 7.59
CHEMBL4876799 — Ki = 1513.56 nM 5.82
CHEMBL4846201 — Ki = 2290.87 nM 5.64
CHEMBL4853107 — Ki = 3235.94 nM 5.49
CHEMBL4878215 — Ki = 3311.31 nM 5.48
CHEMBL4853668 — Ki = 5623.41 nM 5.25
CHEMBL4857560 — Ki = 7413.1 nM 5.13
CHEMBL4871482 — Ki = 7943.28 nM 5.10
CHEMBL4865765 — Ki = 9120.11 nM 5.04
CHEMBL4876025 — Ki = 9120.11 nM 5.04
CHEMBL4846638 — Ki = 10000.0 nM 5.00
CHEMBL4866734 — Ki = 10000.0 nM 5.00
CHEMBL4860528 — Ki = 10471.29 nM 4.98
CHEMBL4872375 — Ki = 10964.78 nM 4.96
CHEMBL4856572 — Ki = 11748.98 nM 4.93
CHEMBL4876267 — Ki = 12882.5 nM 4.89
CHEMBL4863523 — Ki = 14454.4 nM 4.84
CHEMBL4848815 — Ki = 16595.87 nM 4.78
CHEMBL4852212 — Ki = 16982.44 nM 4.77
CHEMBL4863347 — Ki = 17782.79 nM 4.75
CHEMBL4858849 — Ki = 19054.61 nM 4.72
CHEMBL4856005 — Ki = 19498.45 nM 4.71
CHEMBL4870510 — Ki = 21877.62 nM 4.66
CHEMBL4848697 — Ki = 25703.96 nM 4.59
CHEMBL4869194 — Ki = 26302.68 nM 4.58
CHEMBL4869389 — Ki = 26915.35 nM 4.57
CHEMBL4864852 — Ki = 30902.95 nM 4.51
CHEMBL4850448 — Ki = 31622.78 nM 4.50
CHEMBL4867962 — Ki = 33113.11 nM 4.48
CHEMBL4848026 — Ki = 33113.11 nM 4.48
CHEMBL4875600 — Ki = 38904.51 nM 4.41
CHEMBL4856602 — Ki = 43651.58 nM 4.36
CHEMBL4856059 — Ki = 43651.58 nM 4.36
CHEMBL4846380 — Ki = 43651.58 nM 4.36
CHEMBL4874758 — Ki = 44668.36 nM 4.35
CHEMBL4856200 — Ki = 46773.51 nM 4.33
CHEMBL4861704 — Ki = 58884.37 nM 4.23
CHEMBL4853772 — Ki = 64565.42 nM 4.19
CHEMBL4850490 — Ki = 69183.1 nM 4.16
CHEMBL4865965 — Ki = 74131.02 nM 4.13
CHEMBL4854278 — Ki = 81283.05 nM 4.09
CHEMBL4845733 — Ki = 83176.38 nM 4.08
CHEMBL4858567 — pKi - — -
CHEMBL4865670 — pKi - — -
CHEMBL4864067 — pKi - — -
CHEMBL4874969 — pKi - — -
CHEMBL4863393 — pKi - — -
CHEMBL4872277 — pKi - — -
CHEMBL4871221 — pKi - — -
CHEMBL249420 DEXPRAMIPEXOLE pKi - — -