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Assay Detail

CHEMBL898016

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Binding
Inhibition of Tpl2 kinase assessed as MEK phosphorylation by ELISA
ChEMBL ↗
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Identification of a novel class of selective Tpl2 kinase inhibitors: 4-Alkylamino-[1,7]naphthyridine-3-carbonitriles.
Kaila N, Green N, Li HQ, Hu Y, Janz K, Gavrin LK, Thomason J, Tam S, Powell D, Cuozzo J, Hall JP, Telliez JB, Hsu S, Nickerson-Nutter C, Wang Q, Lin LL.
Bioorg Med Chem (2007) 15 : 6425 -6442
PubMed 17664070 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 5.85 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL236808 — — 1 7.75
CHEMBL220037 — — 1 7.72
CHEMBL200381 — — 1 7.30
CHEMBL199230 — — 1 7.30
CHEMBL236384 — — 1 6.80
CHEMBL238326 — — 1 6.60
CHEMBL391358 — — 1 6.57
CHEMBL238323 — — 1 6.50
CHEMBL238273 — — 1 6.44
CHEMBL371095 — — 1 6.42
CHEMBL238322 — — 1 6.40
CHEMBL393707 — — 1 6.33
CHEMBL236383 — — 1 6.20
CHEMBL269242 — — 1 6.04
CHEMBL221330 — — 1 6.00
CHEMBL236982 — — 1 5.89
CHEMBL236810 — — 1 5.89
CHEMBL197538 — — 1 5.82
CHEMBL236985 — — 1 5.80
CHEMBL237462 — — 1 5.80
CHEMBL397305 — — 1 5.77
CHEMBL236811 — — 1 5.77
CHEMBL237460 — — 1 5.66
CHEMBL238264 — — 1 5.62
CHEMBL235768 — — 1 5.58
CHEMBL446633 — — 1 5.55
CHEMBL236983 — — 1 5.54
CHEMBL237461 — — 1 5.54
CHEMBL236981 — — 1 5.52
CHEMBL394916 — — 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL236808 — IC50 = 18.0 nM 7.75
CHEMBL220037 — IC50 = 19.0 nM 7.72
CHEMBL199230 — IC50 = 50.0 nM 7.30
CHEMBL200381 — IC50 = 50.0 nM 7.30
CHEMBL236384 — IC50 = 160.0 nM 6.80
CHEMBL238326 — IC50 = 250.0 nM 6.60
CHEMBL391358 — IC50 = 270.0 nM 6.57
CHEMBL238323 — IC50 = 320.0 nM 6.50
CHEMBL238273 — IC50 = 360.0 nM 6.44
CHEMBL371095 — IC50 = 380.0 nM 6.42
CHEMBL238322 — IC50 = 400.0 nM 6.40
CHEMBL393707 — IC50 = 470.0 nM 6.33
CHEMBL236383 — IC50 = 630.0 nM 6.20
CHEMBL269242 — IC50 = 920.0 nM 6.04
CHEMBL221330 — IC50 = 1000.0 nM 6.00
CHEMBL236982 — IC50 = 1300.0 nM 5.89
CHEMBL236810 — IC50 = 1300.0 nM 5.89
CHEMBL197538 — IC50 = 1500.0 nM 5.82
CHEMBL236985 — IC50 = 1600.0 nM 5.80
CHEMBL237462 — IC50 = 1600.0 nM 5.80
CHEMBL397305 — IC50 = 1700.0 nM 5.77
CHEMBL236811 — IC50 = 1700.0 nM 5.77
CHEMBL237460 — IC50 = 2200.0 nM 5.66
CHEMBL238264 — IC50 = 2400.0 nM 5.62
CHEMBL235768 — IC50 = 2600.0 nM 5.58
CHEMBL446633 — IC50 = 2800.0 nM 5.55
CHEMBL236983 — IC50 = 2900.0 nM 5.54
CHEMBL237461 — IC50 = 2900.0 nM 5.54
CHEMBL236981 — IC50 = 3000.0 nM 5.52
CHEMBL394916 — IC50 = 3000.0 nM 5.52
CHEMBL238318 — IC50 = 3600.0 nM 5.44
CHEMBL235980 — IC50 = 5200.0 nM 5.28
CHEMBL238320 — IC50 = 7000.0 nM 5.16
CHEMBL236380 — IC50 = 7100.0 nM 5.15
CHEMBL392300 — IC50 = 7300.0 nM 5.14
CHEMBL236984 — IC50 = 7300.0 nM 5.14
CHEMBL238319 — IC50 = 7600.0 nM 5.12
CHEMBL199000 — IC50 = 7600.0 nM 5.12
CHEMBL235978 — IC50 = 8000.0 nM 5.10
CHEMBL393706 — IC50 = 10700.0 nM 4.97
CHEMBL236382 — IC50 = 11500.0 nM 4.94
CHEMBL444372 — IC50 = 19700.0 nM 4.71
CHEMBL236809 — IC50 = 21000.0 nM 4.68
CHEMBL235979 — IC50 > 40000.0 nM -
CHEMBL238272 — IC50 > 40000.0 nM -
CHEMBL238321 — IC50 > 10000.0 nM -
CHEMBL393942 — IC50 > 10000.0 nM -
CHEMBL236381 — IC50 > 10000.0 nM -
CHEMBL398574 — IC50 > 40000.0 nM -