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Assay Detail

CHEMBL4146929

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Functional
Agonist activity at human NMUR1 expressed in HEK293 cells assessed as induction of IP3 levels using myo-[2-3H(N)]-inositol after 60 mins by SPA-based topcount assay
38
Total Activities
38
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

Neuromedin-U receptor 1 (CHEMBL1075178)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of potent and proteolytically stable human neuromedin U receptor agonists.
De Prins A, Martin C, Van Wanseele Y, Skov LJ, Tömböly C, Tourwé D, Caveliers V, Van Eeckhaut A, Holst B, Rosenkilde MM, Smolders I, Ballet S.
Eur J Med Chem (2018) 144 : 887 -897
PubMed 29329072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 38 7.13 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4169726 1 9.29
CHEMBL4161902 1 8.80
CHEMBL4177021 1 8.40
CHEMBL4175546 1 8.38
CHEMBL4165337 1 8.37
CHEMBL4174679 1 8.29
CHEMBL4165538 1 8.26
CHEMBL4164922 1 8.11
CHEMBL4175315 1 8.09
CHEMBL4172552 1 7.98
CHEMBL4168753 1 7.91
CHEMBL4166161 1 7.73
CHEMBL4169739 1 7.54
CHEMBL3356083 1 7.41
CHEMBL4160825 1 7.38
CHEMBL4175953 1 7.29
CHEMBL4164026 1 7.18
CHEMBL4167677 1 7.11
CHEMBL4169169 1 7.03
CHEMBL4161501 1 7.03
CHEMBL4169824 1 6.86
CHEMBL4171697 1 6.76
CHEMBL4172829 1 6.73
CHEMBL4168351 1 6.72
CHEMBL4162868 1 6.66
CHEMBL4166325 1 6.64
CHEMBL4176785 1 6.56
CHEMBL4176945 1 6.56
CHEMBL4172768 1 6.46
CHEMBL4159176 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4169726 EC50 = 0.51 nM 9.29
CHEMBL4161902 EC50 = 1.6 nM 8.80
CHEMBL4177021 EC50 = 4.0 nM 8.40
CHEMBL4175546 EC50 = 4.2 nM 8.38
CHEMBL4165337 EC50 = 4.3 nM 8.37
CHEMBL4174679 EC50 = 5.1 nM 8.29
CHEMBL4165538 EC50 = 5.5 nM 8.26
CHEMBL4164922 EC50 = 7.7 nM 8.11
CHEMBL4175315 EC50 = 8.1 nM 8.09
CHEMBL4172552 EC50 = 10.4 nM 7.98
CHEMBL4168753 EC50 = 12.3 nM 7.91
CHEMBL4166161 EC50 = 18.6 nM 7.73
CHEMBL4169739 EC50 = 28.8 nM 7.54
CHEMBL3356083 EC50 = 38.9 nM 7.41
CHEMBL4160825 EC50 = 41.4 nM 7.38
CHEMBL4175953 EC50 = 51.0 nM 7.29
CHEMBL4164026 EC50 = 65.8 nM 7.18
CHEMBL4167677 EC50 = 77.9 nM 7.11
CHEMBL4161501 EC50 = 93.0 nM 7.03
CHEMBL4169169 EC50 = 94.5 nM 7.03
CHEMBL4169824 EC50 = 138.9 nM 6.86
CHEMBL4171697 EC50 = 172.2 nM 6.76
CHEMBL4172829 EC50 = 184.9 nM 6.73
CHEMBL4168351 EC50 = 191.7 nM 6.72
CHEMBL4162868 EC50 = 216.6 nM 6.66
CHEMBL4166325 EC50 = 230.0 nM 6.64
CHEMBL4176785 EC50 = 274.6 nM 6.56
CHEMBL4176945 EC50 = 273.2 nM 6.56
CHEMBL4172768 EC50 = 343.4 nM 6.46
CHEMBL4159176 EC50 = 574.4 nM 6.24
CHEMBL4161095 EC50 = 593.7 nM 6.23
CHEMBL4172327 EC50 = 683.7 nM 6.17
CHEMBL3356082 EC50 = 709.4 nM 6.15
CHEMBL4176206 EC50 = 822.7 nM 6.08
CHEMBL4169433 EC50 = 1053.0 nM 5.98
CHEMBL4161037 EC50 = 2271.0 nM 5.64
CHEMBL4164680 EC50 = 3171.0 nM 5.50
CHEMBL4173583 EC50 = 5496.0 nM 5.26