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Assay Detail

CHEMBL5151674

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

Binding
Inhibition of His6-tagged human NIK (330 to 680 residues) S549D mutant expressed in baculovirus-infected Sf9 cells incubated for 30 mins in presence of ATP by ADP-GloTM assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase kinase kinase 14 (CHEMBL5888)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

An Alkynylpyrimidine-Based Covalent Inhibitor That Targets a Unique Cysteine in NF-κB-Inducing Kinase.
Al-Khawaldeh I, Al Yasiri MJ, Aldred GG, Basmadjian C, Bordoni C, Harnor SJ, Heptinstall AB, Hobson SJ, Jennings CE, Khalifa S, Lebraud H, Martin MP, Miller DC, Shrives HJ, de Souza JV, Stewart HL, Temple M, Thomas HD, Totobenazara J, Tucker JA, Tudhope SJ, Wang LZ, Bronowska AK, Cano C, Endicott JA, Golding BT, Hardcastle IR, Hickson I, Wedge SR, Willmore E, Noble MEM, Waring MJ.
J Med Chem (2021) 64 : 10001 -10018
PubMed 34212719 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.47 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3187788 1 8.40
CHEMBL4211840 1 8.00
CHEMBL2334589 1 7.40
CHEMBL5196202 1 6.70
CHEMBL5198459 1 6.60
CHEMBL5175837 1 6.50
CHEMBL5170825 1 5.80
CHEMBL5182375 1 5.80
CHEMBL5196977 1 5.80
CHEMBL5197109 1 5.50
CHEMBL5206628 1 5.20
CHEMBL5198316 1 5.20
CHEMBL5185097 1 4.70
CHEMBL5175595 1 4.60
CHEMBL5182501 1 4.50
CHEMBL5203009 1 4.40
CHEMBL5181977 1 4.40
CHEMBL5194484 1 4.30
CHEMBL5182228 1 4.20
CHEMBL5190943 1 4.10
CHEMBL5190105 1 4.10
CHEMBL5175142 1 4.10
CHEMBL5204146 1 -
CHEMBL5192481 1 -
CHEMBL5190680 1 -
CHEMBL5203081 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3187788 IC50 = 3.981 nM 8.40
CHEMBL4211840 IC50 = 10.0 nM 8.00
CHEMBL2334589 IC50 = 39.81 nM 7.40
CHEMBL5196202 IC50 = 199.53 nM 6.70
CHEMBL5198459 IC50 = 251.19 nM 6.60
CHEMBL5175837 IC50 = 316.23 nM 6.50
CHEMBL5170825 IC50 = 1584.89 nM 5.80
CHEMBL5182375 IC50 = 1584.89 nM 5.80
CHEMBL5196977 IC50 = 1584.89 nM 5.80
CHEMBL5197109 IC50 = 3162.28 nM 5.50
CHEMBL5206628 IC50 = 6309.57 nM 5.20
CHEMBL5198316 IC50 = 6309.57 nM 5.20
CHEMBL5185097 IC50 = 19952.62 nM 4.70
CHEMBL5175595 IC50 = 25118.86 nM 4.60
CHEMBL5182501 IC50 = 31622.78 nM 4.50
CHEMBL5203009 IC50 = 39810.72 nM 4.40
CHEMBL5181977 IC50 = 39810.72 nM 4.40
CHEMBL5194484 IC50 = 50118.72 nM 4.30
CHEMBL5182228 IC50 = 63095.73 nM 4.20
CHEMBL5190943 IC50 = 79432.82 nM 4.10
CHEMBL5190105 IC50 = 79432.82 nM 4.10
CHEMBL5175142 IC50 = 79432.82 nM 4.10
CHEMBL5204146 IC50 = 501187.23 nM -
CHEMBL5192481 IC50 = 501187.23 nM -
CHEMBL5190680 IC50 > 100000.0 nM -
CHEMBL5203081 IC50 = 398107.17 nM -