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Assay Detail

CHEMBL920402

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

Binding
Inhibition of cytokine-induced iNOS expressed in human A172 cells assessed as inhibition of NO formation
ChEMBL ↗
80
Total Activities
80
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A 172
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Nitric oxide synthase, inducible (CHEMBL4481) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and activity of 2-imidazol-1-ylpyrimidine derived inducible nitric oxide synthase dimerization inhibitors.
Davey DD, Adler M, Arnaiz D, Eagen K, Erickson S, Guilford W, Kenrick M, Morrissey MM, Ohlmeyer M, Pan G, Paradkar VM, Parkinson J, Polokoff M, Saionz K, Santos C, Subramanyam B, Vergona R, Wei RG, Whitlow M, Ye B, Zhao ZS, Devlin JJ, Phillips G.
J Med Chem (2007) 50 : 1146 -1157
PubMed 17315988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 80 8.25 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220632 — — 1 9.92
CHEMBL220880 — — 1 9.89
CHEMBL385324 — — 1 9.62
CHEMBL376733 — — 1 9.55
CHEMBL385325 — — 1 9.55
CHEMBL376632 — — 1 9.54
CHEMBL290548 — — 1 9.42
CHEMBL373623 — — 1 9.32
CHEMBL427062 — — 1 9.32
CHEMBL223788 — — 1 9.31
CHEMBL376713 — — 1 9.30
CHEMBL220932 — — 1 9.30
CHEMBL442041 — — 1 9.30
CHEMBL385334 — — 1 9.30
CHEMBL221208 — — 1 9.28
CHEMBL411343 — — 1 9.26
CHEMBL424928 — — 1 9.24
CHEMBL223782 — — 1 9.17
CHEMBL373881 — — 1 9.15
CHEMBL222362 — — 1 9.12
CHEMBL374681 — — 1 9.10
CHEMBL223792 — — 1 9.10
CHEMBL374319 — — 1 9.06
CHEMBL222364 — — 1 9.03
CHEMBL223791 — — 1 9.02
CHEMBL223384 — — 1 9.00
CHEMBL223634 — — 1 9.00
CHEMBL375404 — — 1 9.00
CHEMBL220834 — — 1 9.00
CHEMBL374132 — — 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220632 — IC50 = 0.12 nM 9.92
CHEMBL220880 — IC50 = 0.13 nM 9.89
CHEMBL385324 — IC50 = 0.24 nM 9.62
CHEMBL376733 — IC50 = 0.28 nM 9.55
CHEMBL385325 — IC50 = 0.28 nM 9.55
CHEMBL376632 — IC50 = 0.29 nM 9.54
CHEMBL290548 — IC50 = 0.38 nM 9.42
CHEMBL373623 — IC50 = 0.48 nM 9.32
CHEMBL427062 — IC50 = 0.48 nM 9.32
CHEMBL223788 — IC50 = 0.49 nM 9.31
CHEMBL376713 — IC50 = 0.5 nM 9.30
CHEMBL220932 — IC50 = 0.5 nM 9.30
CHEMBL442041 — IC50 = 0.5 nM 9.30
CHEMBL385334 — IC50 = 0.5 nM 9.30
CHEMBL221208 — IC50 = 0.52 nM 9.28
CHEMBL411343 — IC50 = 0.55 nM 9.26
CHEMBL424928 — IC50 = 0.58 nM 9.24
CHEMBL223782 — IC50 = 0.67 nM 9.17
CHEMBL373881 — IC50 = 0.7 nM 9.15
CHEMBL222362 — IC50 = 0.75 nM 9.12
CHEMBL374681 — IC50 = 0.8 nM 9.10
CHEMBL223792 — IC50 = 0.8 nM 9.10
CHEMBL374319 — IC50 = 0.87 nM 9.06
CHEMBL222364 — IC50 = 0.93 nM 9.03
CHEMBL223791 — IC50 = 0.96 nM 9.02
CHEMBL223384 — IC50 = 1.0 nM 9.00
CHEMBL374132 — IC50 = 1.0 nM 9.00
CHEMBL220834 — IC50 = 1.0 nM 9.00
CHEMBL223634 — IC50 = 1.0 nM 9.00
CHEMBL375404 — IC50 = 1.0 nM 9.00
CHEMBL223838 — IC50 = 1.1 nM 8.96
CHEMBL223385 — IC50 = 1.4 nM 8.85
CHEMBL220121 — IC50 = 1.5 nM 8.82
CHEMBL220771 — IC50 = 1.9 nM 8.72
CHEMBL223442 — IC50 = 2.0 nM 8.70
CHEMBL220156 — IC50 = 2.7 nM 8.57
CHEMBL436535 — IC50 = 3.0 nM 8.52
CHEMBL387348 — IC50 = 3.5 nM 8.46
CHEMBL387349 — IC50 = 3.7 nM 8.43
CHEMBL221264 — IC50 = 4.1 nM 8.39
CHEMBL222619 — IC50 = 5.4 nM 8.27
CHEMBL376237 — IC50 = 5.7 nM 8.24
CHEMBL219792 — IC50 = 8.5 nM 8.07
CHEMBL374552 — IC50 = 10.0 nM 8.00
CHEMBL220559 — IC50 = 11.0 nM 7.96
CHEMBL424756 — IC50 = 12.0 nM 7.92
CHEMBL223615 — IC50 = 12.0 nM 7.92
CHEMBL220122 — IC50 = 12.0 nM 7.92
CHEMBL374300 — IC50 = 17.0 nM 7.77
CHEMBL220270 — IC50 = 19.0 nM 7.72