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Assay Detail

CHEMBL4815471

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

Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
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 H2 receptor (CHEMBL1941) ↗
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 51 6.87 8.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4875600 — — 1 8.69
CHEMBL4860528 — — 1 8.35
CHEMBL4865965 — — 1 7.98
CHEMBL4856059 — — 1 7.75
CHEMBL4853668 — — 1 7.54
CHEMBL4864852 — — 1 7.54
CHEMBL4876267 — — 1 7.52
CHEMBL4869194 — — 1 7.51
CHEMBL4846380 — — 1 7.50
CHEMBL4848697 — — 1 7.50
CHEMBL4858849 — — 1 7.45
CHEMBL4848026 — — 1 7.43
CHEMBL4846638 — — 1 7.40
CHEMBL4876025 — — 1 7.36
CHEMBL4863347 — — 1 7.33
CHEMBL4867962 — — 1 7.29
CHEMBL4846201 — — 1 7.22
CHEMBL4865765 — — 1 7.20
CHEMBL4861704 — — 1 7.20
CHEMBL4870510 — — 1 7.20
CHEMBL4856005 — — 1 7.16
CHEMBL4857560 — — 1 7.15
CHEMBL4853107 — — 1 7.14
CHEMBL4848815 — — 1 7.11
CHEMBL4866734 — — 1 7.06
CHEMBL4852212 — — 1 7.00
CHEMBL4869389 — — 1 6.99
CHEMBL4856572 — — 1 6.99
CHEMBL4874758 — — 1 6.98
CHEMBL4853772 — — 1 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4875600 — Ki = 2.042 nM 8.69
CHEMBL4860528 — Ki = 4.467 nM 8.35
CHEMBL4865965 — Ki = 10.47 nM 7.98
CHEMBL4856059 — Ki = 17.78 nM 7.75
CHEMBL4853668 — Ki = 28.84 nM 7.54
CHEMBL4864852 — Ki = 28.84 nM 7.54
CHEMBL4876267 — Ki = 30.2 nM 7.52
CHEMBL4869194 — Ki = 30.9 nM 7.51
CHEMBL4846380 — Ki = 31.62 nM 7.50
CHEMBL4848697 — Ki = 31.62 nM 7.50
CHEMBL4858849 — Ki = 35.48 nM 7.45
CHEMBL4848026 — Ki = 37.15 nM 7.43
CHEMBL4846638 — Ki = 39.81 nM 7.40
CHEMBL4876025 — Ki = 43.65 nM 7.36
CHEMBL4863347 — Ki = 46.77 nM 7.33
CHEMBL4867962 — Ki = 51.29 nM 7.29
CHEMBL4846201 — Ki = 60.26 nM 7.22
CHEMBL4865765 — Ki = 63.1 nM 7.20
CHEMBL4861704 — Ki = 63.1 nM 7.20
CHEMBL4870510 — Ki = 63.1 nM 7.20
CHEMBL4856005 — Ki = 69.18 nM 7.16
CHEMBL4857560 — Ki = 70.79 nM 7.15
CHEMBL4853107 — Ki = 72.44 nM 7.14
CHEMBL4848815 — Ki = 77.62 nM 7.11
CHEMBL4866734 — Ki = 87.1 nM 7.06
CHEMBL4852212 — Ki = 100.0 nM 7.00
CHEMBL4856572 — Ki = 102.33 nM 6.99
CHEMBL4869389 — Ki = 102.33 nM 6.99
CHEMBL4874758 — Ki = 104.71 nM 6.98
CHEMBL4853772 — Ki = 114.82 nM 6.94
CHEMBL4863523 — Ki = 125.89 nM 6.90
CHEMBL4871482 — Ki = 147.91 nM 6.83
CHEMBL4864067 — Ki = 158.49 nM 6.80
CHEMBL4876743 — Ki = 169.82 nM 6.77
CHEMBL4850448 — Ki = 229.09 nM 6.64
CHEMBL90 HISTAMINE Ki = 263.03 nM 6.58
CHEMBL4854278 — Ki = 338.84 nM 6.47
CHEMBL4845733 — Ki = 426.58 nM 6.37
CHEMBL4878215 — Ki = 512.86 nM 6.29
CHEMBL4856602 — Ki = 602.56 nM 6.22
CHEMBL4872375 — Ki = 691.83 nM 6.16
CHEMBL4876799 — Ki = 1122.02 nM 5.95
CHEMBL4850490 — Ki = 1148.15 nM 5.94
CHEMBL4856200 — Ki = 1445.44 nM 5.84
CHEMBL4872277 — Ki = 1995.26 nM 5.70
CHEMBL4858567 — Ki = 3162.28 nM 5.50
CHEMBL4871221 — Ki = 3981.07 nM 5.40
CHEMBL4874969 — Ki = 4466.84 nM 5.35
CHEMBL4865670 — Ki = 5248.07 nM 5.28
CHEMBL249420 DEXPRAMIPEXOLE Ki = 13803.84 nM 4.86