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Assay Detail

CHEMBL4815470

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

Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 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 H1 receptor (CHEMBL231) ↗
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 4.99 5.92
pKi 9 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4878215 — — 1 5.92
CHEMBL4865765 — — 1 5.87
CHEMBL4853107 — — 1 5.78
CHEMBL4876799 — — 1 5.71
CHEMBL4846638 — — 1 5.63
CHEMBL90 HISTAMINE 4.0 1 5.62
CHEMBL4876267 — — 1 5.54
CHEMBL4857560 — — 1 5.42
CHEMBL4863347 — — 1 5.35
CHEMBL4871482 — — 1 5.31
CHEMBL4869194 — — 1 5.29
CHEMBL4866734 — — 1 5.28
CHEMBL4856572 — — 1 5.23
CHEMBL4848026 — — 1 5.23
CHEMBL4856005 — — 1 5.21
CHEMBL4846201 — — 1 5.15
CHEMBL4853668 — — 1 5.11
CHEMBL4875600 — — 1 5.11
CHEMBL4848815 — — 1 5.10
CHEMBL4856059 — — 1 5.06
CHEMBL4852212 — — 1 5.06
CHEMBL4869389 — — 1 5.02
CHEMBL4848697 — — 1 4.99
CHEMBL4860528 — — 1 4.97
CHEMBL4870510 — — 1 4.90
CHEMBL4876025 — — 1 4.80
CHEMBL4864852 — — 1 4.77
CHEMBL4867962 — — 1 4.67
CHEMBL4863523 — — 1 4.66
CHEMBL4865965 — — 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4878215 — Ki = 1202.26 nM 5.92
CHEMBL4865765 — Ki = 1348.96 nM 5.87
CHEMBL4853107 — Ki = 1659.59 nM 5.78
CHEMBL4876799 — Ki = 1949.84 nM 5.71
CHEMBL4846638 — Ki = 2344.23 nM 5.63
CHEMBL90 HISTAMINE Ki = 2398.83 nM 5.62
CHEMBL4876267 — Ki = 2884.03 nM 5.54
CHEMBL4857560 — Ki = 3801.89 nM 5.42
CHEMBL4863347 — Ki = 4466.84 nM 5.35
CHEMBL4871482 — Ki = 4897.79 nM 5.31
CHEMBL4869194 — Ki = 5128.61 nM 5.29
CHEMBL4866734 — Ki = 5248.07 nM 5.28
CHEMBL4856572 — Ki = 5888.44 nM 5.23
CHEMBL4848026 — Ki = 5888.44 nM 5.23
CHEMBL4856005 — Ki = 6165.95 nM 5.21
CHEMBL4846201 — Ki = 7079.46 nM 5.15
CHEMBL4853668 — Ki = 7762.47 nM 5.11
CHEMBL4875600 — Ki = 7762.47 nM 5.11
CHEMBL4848815 — Ki = 7943.28 nM 5.10
CHEMBL4856059 — Ki = 8709.64 nM 5.06
CHEMBL4852212 — Ki = 8709.64 nM 5.06
CHEMBL4869389 — Ki = 9549.93 nM 5.02
CHEMBL4848697 — Ki = 10232.93 nM 4.99
CHEMBL4860528 — Ki = 10715.19 nM 4.97
CHEMBL4870510 — Ki = 12589.25 nM 4.90
CHEMBL4876025 — Ki = 15848.93 nM 4.80
CHEMBL4864852 — Ki = 16982.44 nM 4.77
CHEMBL4867962 — Ki = 21379.62 nM 4.67
CHEMBL4863523 — Ki = 21877.62 nM 4.66
CHEMBL4865965 — Ki = 23988.33 nM 4.62
CHEMBL4858849 — Ki = 24547.09 nM 4.61
CHEMBL4876743 — Ki = 24547.09 nM 4.61
CHEMBL4861704 — Ki = 25703.96 nM 4.59
CHEMBL4874758 — Ki = 28840.32 nM 4.54
CHEMBL4856200 — Ki = 44668.36 nM 4.35
CHEMBL4846380 — Ki = 45708.82 nM 4.34
CHEMBL4856602 — Ki = 46773.51 nM 4.33
CHEMBL4845733 — Ki = 52480.75 nM 4.28
CHEMBL4850448 — Ki = 53703.18 nM 4.27
CHEMBL4850490 — Ki = 63095.73 nM 4.20
CHEMBL4854278 — Ki = 77624.71 nM 4.11
CHEMBL4858567 — pKi - — -
CHEMBL4853772 — Ki = 109647.82 nM -
CHEMBL4865670 — pKi - — -
CHEMBL4872375 — pKi - — -
CHEMBL4874969 — pKi - — -
CHEMBL4863393 — pKi - — -
CHEMBL4872277 — pKi - — -
CHEMBL4871221 — pKi - — -
CHEMBL4864067 — pKi - — -