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Assay Detail

CHEMBL1827500

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

Functional
Inverse agonist activity at HCMV TB40/E US28 expressed in human HEK cells assessed as Elk-1 activation preincubated for 1 hrs measured after 20 to 24 hrs by luciferase reporter gene assay
41
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human betaherpesvirus 5
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification of novel allosteric modulators for the G-protein coupled US28 receptor of human cytomegalovirus.
Kralj A, Wetzel A, Mahmoudian S, Stamminger T, Tschammer N, Heinrich MR.
Bioorg Med Chem Lett (2011) 21 : 5446 -5450
PubMed 21784633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 41 5.65 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1824282 2 6.89
CHEMBL1824267 2 6.56
CHEMBL93240 METITEPINE 2.0 2 6.46
CHEMBL1824272 2 6.00
CHEMBL1824284 2 5.85
CHEMBL1824269 2 5.82
CHEMBL1824498 2 5.82
CHEMBL1824279 2 5.75
CHEMBL1824280 2 5.70
CHEMBL1821755 2 5.64
CHEMBL1824275 2 5.47
CHEMBL1824270 2 5.36
CHEMBL34166 BERLEX COMPOUND 2 5.35
CHEMBL1824268 2 5.32
CHEMBL1824274 2 5.13
CHEMBL1824278 2 5.12
CHEMBL1824281 2 5.11
CHEMBL1824273 2 5.07
CHEMBL1824276 2 4.87
CHEMBL1824271 1 -
CHEMBL1824277 1 -
CHEMBL1824283 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1824282 EC50 = 128.82 nM 6.89
CHEMBL1824282 EC50 = 130.0 nM 6.89
CHEMBL1824267 EC50 = 275.42 nM 6.56
CHEMBL1824267 EC50 = 280.0 nM 6.55
CHEMBL93240 METITEPINE EC50 = 350.0 nM 6.46
CHEMBL93240 METITEPINE EC50 = 354.81 nM 6.45
CHEMBL1824272 EC50 = 1000.0 nM 6.00
CHEMBL1824272 EC50 = 1023.29 nM 5.99
CHEMBL1824284 EC50 = 1400.0 nM 5.85
CHEMBL1824284 EC50 = 1412.54 nM 5.85
CHEMBL1824269 EC50 = 1513.56 nM 5.82
CHEMBL1824498 EC50 = 1500.0 nM 5.82
CHEMBL1824269 EC50 = 1500.0 nM 5.82
CHEMBL1824498 EC50 = 1548.82 nM 5.81
CHEMBL1824279 EC50 = 1800.0 nM 5.75
CHEMBL1824279 EC50 = 1778.28 nM 5.75
CHEMBL1824280 EC50 = 2000.0 nM 5.70
CHEMBL1824280 EC50 = 1995.26 nM 5.70
CHEMBL1821755 EC50 = 2300.0 nM 5.64
CHEMBL1821755 EC50 = 2290.87 nM 5.64
CHEMBL1824275 EC50 = 3400.0 nM 5.47
CHEMBL1824275 EC50 = 3467.37 nM 5.46
CHEMBL1824270 EC50 = 4400.0 nM 5.36
CHEMBL1824270 EC50 = 4365.16 nM 5.36
CHEMBL34166 BERLEX COMPOUND EC50 = 4500.0 nM 5.35
CHEMBL34166 BERLEX COMPOUND EC50 = 4570.88 nM 5.34
CHEMBL1824268 EC50 = 4786.3 nM 5.32
CHEMBL1824268 EC50 = 4800.0 nM 5.32
CHEMBL1824274 EC50 = 7413.1 nM 5.13
CHEMBL1824274 EC50 = 7400.0 nM 5.13
CHEMBL1824278 EC50 = 7500.0 nM 5.12
CHEMBL1824278 EC50 = 7585.78 nM 5.12
CHEMBL1824281 EC50 = 7762.47 nM 5.11
CHEMBL1824281 EC50 = 7800.0 nM 5.11
CHEMBL1824273 EC50 = 8511.38 nM 5.07
CHEMBL1824273 EC50 = 8500.0 nM 5.07
CHEMBL1824276 EC50 = 13489.63 nM 4.87
CHEMBL1824276 EC50 = 13500.0 nM 4.87
CHEMBL1824271 EC50 - -
CHEMBL1824277 EC50 - -
CHEMBL1824283 EC50 - -