Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4154306

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

Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL ↗
44
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification of novel β-lactams and pyrrolidinone derivatives as selective Histamine-3 receptor (H3R) modulators as possible anti-obesity agents.
Ghoshal A, Kumar A, Yugandhar D, Sona C, Kuriakose S, Nagesh K, Rashid M, Singh SK, Wahajuddin M, Yadav PN, Srivastava AK.
Eur J Med Chem (2018) 152 : 148 -159
PubMed 29704723 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 44 8.41 10.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1490875 — — 2 10.16
CHEMBL4170869 — — 2 10.00
CHEMBL4159570 — — 2 10.00
CHEMBL4159472 — — 2 9.58
CHEMBL4177416 — — 2 9.57
CHEMBL4162793 — — 2 8.96
CHEMBL4165989 — — 2 8.91
CHEMBL4164467 — — 2 8.89
CHEMBL4166098 — — 2 8.57
CHEMBL4175898 — — 2 8.57
CHEMBL4166386 — — 2 8.52
CHEMBL4175106 — — 2 8.42
CHEMBL4176601 — — 2 8.25
CHEMBL4165167 — — 2 8.18
CHEMBL4174591 — — 2 8.00
CHEMBL4161732 — — 2 7.89
CHEMBL4169663 — — 2 7.84
CHEMBL4174766 — — 2 7.62
CHEMBL4167482 — — 2 7.21
CHEMBL4166675 — — 2 7.03
CHEMBL4166645 — — 2 6.98
CHEMBL4174017 — — 2 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1490875 — EC50 = 0.06918 nM 10.16
CHEMBL1490875 — EC50 = 0.08 nM 10.10
CHEMBL4159570 — EC50 = 0.1 nM 10.00
CHEMBL4170869 — EC50 = 0.1 nM 10.00
CHEMBL4159570 — EC50 = 0.123 nM 9.91
CHEMBL4170869 — EC50 = 0.1318 nM 9.88
CHEMBL4159472 — EC50 = 0.263 nM 9.58
CHEMBL4177416 — EC50 = 0.2692 nM 9.57
CHEMBL4177416 — EC50 = 0.3 nM 9.52
CHEMBL4159472 — EC50 = 0.3 nM 9.52
CHEMBL4162793 — EC50 = 1.1 nM 8.96
CHEMBL4162793 — EC50 = 1.122 nM 8.95
CHEMBL4165989 — EC50 = 1.23 nM 8.91
CHEMBL4164467 — EC50 = 1.3 nM 8.89
CHEMBL4164467 — EC50 = 1.288 nM 8.89
CHEMBL4165989 — EC50 = 1.3 nM 8.89
CHEMBL4175898 — EC50 = 2.7 nM 8.57
CHEMBL4166098 — EC50 = 2.692 nM 8.57
CHEMBL4166098 — EC50 = 2.7 nM 8.57
CHEMBL4175898 — EC50 = 2.754 nM 8.56
CHEMBL4166386 — EC50 = 3.0 nM 8.52
CHEMBL4175106 — EC50 = 3.8 nM 8.42
CHEMBL4175106 — EC50 = 3.802 nM 8.42
CHEMBL4176601 — EC50 = 5.623 nM 8.25
CHEMBL4176601 — EC50 = 5.7 nM 8.24
CHEMBL4165167 — EC50 = 6.607 nM 8.18
CHEMBL4165167 — EC50 = 6.7 nM 8.17
CHEMBL4174591 — EC50 = 10.0 nM 8.00
CHEMBL4174591 — EC50 = 10.23 nM 7.99
CHEMBL4161732 — EC50 = 13.0 nM 7.89
CHEMBL4161732 — EC50 = 13.49 nM 7.87
CHEMBL4169663 — EC50 = 14.4 nM 7.84
CHEMBL4169663 — EC50 = 14.45 nM 7.84
CHEMBL4166386 — EC50 = 22.91 nM 7.64
CHEMBL4174766 — EC50 = 24.0 nM 7.62
CHEMBL4174766 — EC50 = 25.7 nM 7.59
CHEMBL4167482 — EC50 = 61.66 nM 7.21
CHEMBL4166675 — EC50 = 94.0 nM 7.03
CHEMBL4166675 — EC50 = 93.33 nM 7.03
CHEMBL4167482 — EC50 = 104.0 nM 6.98
CHEMBL4166645 — EC50 = 104.71 nM 6.98
CHEMBL4166645 — EC50 = 104.0 nM 6.98
CHEMBL4174017 — EC50 = 186.21 nM 6.73
CHEMBL4174017 — EC50 = 187.0 nM 6.73