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Assay Detail

CHEMBL1937261

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Functional
Inhibition of LPS-induced TNFalpha production in human THP1 cells pre-incubated for 30 mins prior to LPS-induction measured after 4 hrs by ELISA
ChEMBL ↗
40
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 1 — Organism
Curated By Autocuration

Target

THP-1 (CHEMBL614245) ↗
Type CELL-LINE
Organism Homo sapiens

Publication

Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series.
Oubrie A, Kaptein A, de Zwart E, Hoogenboom N, Goorden R, van de Kar B, van Hoek M, de Kimpe V, van der Heijden R, Borsboom J, Kazemier B, de Roos J, Scheffers M, Lommerse J, Schultz-Fademrecht C, Barf T.
Bioorg Med Chem Lett (2012) 22 : 613 -618
PubMed 22119462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 40 6.10 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1933173 — — 1 7.10
CHEMBL1933180 — — 1 6.66
CHEMBL1933162 — — 1 6.64
CHEMBL1933181 — — 3 6.51
CHEMBL1933164 — — 1 6.50
CHEMBL1933188 — — 1 6.47
CHEMBL1933178 — — 3 6.34
CHEMBL1933185 — — 1 6.32
CHEMBL1933166 — — 1 6.31
CHEMBL1933179 — — 3 6.29
CHEMBL1933172 — — 1 6.27
CHEMBL1933182 — — 1 6.25
CHEMBL1933183 — — 1 6.21
CHEMBL1933175 — — 1 6.18
CHEMBL1933192 — — 1 6.16
CHEMBL1933169 — — 1 6.14
CHEMBL1933176 — — 1 6.14
CHEMBL1933171 — — 1 6.11
CHEMBL1933187 — — 1 6.07
CHEMBL1738702 — — 1 6.04
CHEMBL1933174 — — 1 6.00
CHEMBL1933191 — — 1 5.96
CHEMBL1933186 — — 1 5.96
CHEMBL1933170 — — 1 5.96
CHEMBL1933190 — — 1 5.96
CHEMBL1933168 — — 1 5.89
CHEMBL1933184 — — 1 5.89
CHEMBL1933189 — — 1 5.77
CHEMBL1933163 — — 1 5.47
CHEMBL1933161 — — 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1933173 — EC50 = 80.0 nM 7.10
CHEMBL1933180 — EC50 = 220.0 nM 6.66
CHEMBL1933162 — EC50 = 230.0 nM 6.64
CHEMBL1933181 — EC50 = 310.0 nM 6.51
CHEMBL1933164 — EC50 = 320.0 nM 6.50
CHEMBL1933181 — EC50 = 320.0 nM 6.50
CHEMBL1933188 — EC50 = 340.0 nM 6.47
CHEMBL1933178 — EC50 = 460.0 nM 6.34
CHEMBL1933185 — EC50 = 480.0 nM 6.32
CHEMBL1933166 — EC50 = 490.0 nM 6.31
CHEMBL1933179 — EC50 = 510.0 nM 6.29
CHEMBL1933172 — EC50 = 540.0 nM 6.27
CHEMBL1933182 — EC50 = 560.0 nM 6.25
CHEMBL1933183 — EC50 = 620.0 nM 6.21
CHEMBL1933178 — EC50 = 650.0 nM 6.19
CHEMBL1933175 — EC50 = 660.0 nM 6.18
CHEMBL1933192 — EC50 = 690.0 nM 6.16
CHEMBL1933169 — EC50 = 720.0 nM 6.14
CHEMBL1933176 — EC50 = 720.0 nM 6.14
CHEMBL1933171 — EC50 = 780.0 nM 6.11
CHEMBL1933179 — EC50 = 780.0 nM 6.11
CHEMBL1933187 — EC50 = 850.0 nM 6.07
CHEMBL1738702 — EC50 = 910.0 nM 6.04
CHEMBL1933174 — EC50 = 1000.0 nM 6.00
CHEMBL1933186 — EC50 = 1100.0 nM 5.96
CHEMBL1933170 — EC50 = 1100.0 nM 5.96
CHEMBL1933190 — EC50 = 1100.0 nM 5.96
CHEMBL1933191 — EC50 = 1100.0 nM 5.96
CHEMBL1933184 — EC50 = 1300.0 nM 5.89
CHEMBL1933168 — EC50 = 1300.0 nM 5.89
CHEMBL1933189 — EC50 = 1700.0 nM 5.77
CHEMBL1933161 — EC50 = 3400.0 nM 5.47
CHEMBL1933163 — EC50 = 3400.0 nM 5.47
CHEMBL1933193 — EC50 = 3900.0 nM 5.41
CHEMBL1933167 — EC50 = 7900.0 nM 5.10
CHEMBL1933178 — EC50 = 8500.0 nM 5.07
CHEMBL1933179 — EC50 - — -
CHEMBL1933165 — EC50 > 10000.0 nM -
CHEMBL1933181 — EC50 > 10000.0 nM -
CHEMBL1933177 — EC50 > 10000.0 nM -