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Assay Detail

CHEMBL944092

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Functional
Activation of SMN2 promoter in mouse NSC34 cells assessed as induction of beta-lactamase activity
ChEMBL ↗
114
Total Activities
113
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type NSC34
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Synthesis and biological evaluation of novel 2,4-diaminoquinazoline derivatives as SMN2 promoter activators for the potential treatment of spinal muscular atrophy.
Thurmond J, Butchbach ME, Palomo M, Pease B, Rao M, Bedell L, Keyvan M, Pai G, Mishra R, Haraldsson M, Andresson T, Bragason G, Thosteinsdottir M, Bjornsson JM, Coovert DD, Burghes AH, Gurney ME, Singh J.
J Med Chem (2008) 51 : 449 -469
PubMed 18205293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 114 6.85 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL253976 — — 1 8.70
CHEMBL251429 — — 1 8.40
CHEMBL251657 — — 1 7.85
CHEMBL398675 — — 1 7.85
CHEMBL251632 — — 1 7.80
CHEMBL84108 — — 1 7.77
CHEMBL1203957 — — 1 7.75
CHEMBL250245 — — 1 7.75
CHEMBL254182 — — 1 7.75
CHEMBL251906 — — 1 7.72
CHEMBL398416 — — 1 7.68
CHEMBL250246 — — 1 7.66
CHEMBL249256 — — 1 7.64
CHEMBL1203956 — — 1 7.62
CHEMBL249636 — — 1 7.62
CHEMBL251434 — — 1 7.54
CHEMBL253975 — — 1 7.50
CHEMBL250076 — — 1 7.46
CHEMBL254181 — — 1 7.46
CHEMBL400348 — — 1 7.42
CHEMBL250072 — — 1 7.42
CHEMBL400452 — — 1 7.40
CHEMBL251428 — — 1 7.38
CHEMBL255019 — — 1 7.38
CHEMBL250074 — — 1 7.37
CHEMBL250073 — — 1 7.33
CHEMBL253977 — — 1 7.33
CHEMBL429304 — — 1 7.33
CHEMBL250075 — — 1 7.31
CHEMBL398613 — — 2 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL253976 — EC50 = 2.0 nM 8.70
CHEMBL251429 — EC50 = 4.0 nM 8.40
CHEMBL398675 — EC50 = 14.0 nM 7.85
CHEMBL251657 — EC50 = 14.0 nM 7.85
CHEMBL251632 — EC50 = 16.0 nM 7.80
CHEMBL84108 — EC50 = 17.0 nM 7.77
CHEMBL254182 — EC50 = 18.0 nM 7.75
CHEMBL1203957 — EC50 = 18.0 nM 7.75
CHEMBL250245 — EC50 = 18.0 nM 7.75
CHEMBL251906 — EC50 = 19.0 nM 7.72
CHEMBL398416 — EC50 = 21.0 nM 7.68
CHEMBL250246 — EC50 = 22.0 nM 7.66
CHEMBL249256 — EC50 = 23.0 nM 7.64
CHEMBL249636 — EC50 = 24.0 nM 7.62
CHEMBL1203956 — EC50 = 24.0 nM 7.62
CHEMBL251434 — EC50 = 29.0 nM 7.54
CHEMBL253975 — EC50 = 32.0 nM 7.50
CHEMBL254181 — EC50 = 35.0 nM 7.46
CHEMBL250076 — EC50 = 35.0 nM 7.46
CHEMBL400348 — EC50 = 38.0 nM 7.42
CHEMBL250072 — EC50 = 38.0 nM 7.42
CHEMBL400452 — EC50 = 40.0 nM 7.40
CHEMBL255019 — EC50 = 42.0 nM 7.38
CHEMBL251428 — EC50 = 42.0 nM 7.38
CHEMBL250074 — EC50 = 43.0 nM 7.37
CHEMBL429304 — EC50 = 47.0 nM 7.33
CHEMBL250073 — EC50 = 47.0 nM 7.33
CHEMBL253977 — EC50 = 47.0 nM 7.33
CHEMBL250075 — EC50 = 49.0 nM 7.31
CHEMBL400062 — EC50 = 50.0 nM 7.30
CHEMBL398613 — EC50 = 50.0 nM 7.30
CHEMBL251427 — EC50 = 52.0 nM 7.28
CHEMBL251286 — EC50 = 53.0 nM 7.28
CHEMBL251430 — EC50 = 54.0 nM 7.27
CHEMBL400672 — EC50 = 55.0 nM 7.26
CHEMBL398613 — EC50 = 55.0 nM 7.26
CHEMBL254804 — EC50 = 60.0 nM 7.22
CHEMBL413990 — EC50 = 60.0 nM 7.22
CHEMBL251449 — EC50 = 65.0 nM 7.19
CHEMBL251630 — EC50 = 66.0 nM 7.18
CHEMBL251264 — EC50 = 67.0 nM 7.17
CHEMBL249648 — EC50 = 73.0 nM 7.14
CHEMBL251432 — EC50 = 74.0 nM 7.13
CHEMBL250231 — EC50 = 78.0 nM 7.11
CHEMBL398417 — EC50 = 80.0 nM 7.10
CHEMBL250079 — EC50 = 82.0 nM 7.09
CHEMBL438698 — EC50 = 81.0 nM 7.09
CHEMBL402486 — EC50 = 89.0 nM 7.05
CHEMBL253761 — EC50 = 97.0 nM 7.01
CHEMBL251263 — EC50 = 104.0 nM 6.98