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Assay Detail

CHEMBL751415

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

Functional
Cytotoxicity against human non-small-cell lung carcinoma cell line H460 (NSCLC-H460)
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type carcinoma cell line
Confidence 1 — Organism
Curated By Autocuration

Publication

Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
Dallavalle S, Ferrari A, Biasotti B, Merlini L, Penco S, Gallo G, Marzi M, Tinti MO, Martinelli R, Pisano C, Carminati P, Carenini N, Beretta G, Perego P, De Cesare M, Pratesi G, Zunino F.
J Med Chem (2001) 44 : 3264 -3274
PubMed 11563925 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 6.62 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113051 GIMATECAN 2.0 1 7.82
CHEMBL424435 1 7.77
CHEMBL323422 1 7.70
CHEMBL324202 1 7.70
CHEMBL112308 1 7.60
CHEMBL322811 1 7.55
CHEMBL111767 1 7.52
CHEMBL326907 1 7.52
CHEMBL326720 1 7.50
CHEMBL111012 1 7.40
CHEMBL112962 1 7.22
CHEMBL109359 1 7.16
CHEMBL325393 1 7.16
CHEMBL325254 1 7.10
CHEMBL837 7-ETHYL-10-HYDROXYCAMPTOTHECIN 2.0 1 7.10
CHEMBL323751 1 7.00
CHEMBL112769 1 6.89
CHEMBL322337 1 6.89
CHEMBL111209 1 6.85
CHEMBL113482 1 6.80
CHEMBL320127 1 6.70
CHEMBL112334 1 6.68
CHEMBL113558 1 6.55
CHEMBL113393 1 6.52
CHEMBL65 CAMPTOTHECIN -1.0 1 6.48
CHEMBL114135 1 6.47
CHEMBL3215370 1 6.44
CHEMBL419186 1 6.31
CHEMBL322141 1 6.30
CHEMBL84 TOPOTECAN 4.0 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113051 GIMATECAN IC50 = 15.0 nM 7.82
CHEMBL424435 IC50 = 17.0 nM 7.77
CHEMBL324202 IC50 = 20.0 nM 7.70
CHEMBL323422 IC50 = 20.0 nM 7.70
CHEMBL112308 IC50 = 25.0 nM 7.60
CHEMBL322811 IC50 = 28.0 nM 7.55
CHEMBL111767 IC50 = 30.0 nM 7.52
CHEMBL326907 IC50 = 30.0 nM 7.52
CHEMBL326720 IC50 = 32.0 nM 7.50
CHEMBL111012 IC50 = 40.0 nM 7.40
CHEMBL112962 IC50 = 60.0 nM 7.22
CHEMBL109359 IC50 = 70.0 nM 7.16
CHEMBL325393 IC50 = 70.0 nM 7.16
CHEMBL325254 IC50 = 80.0 nM 7.10
CHEMBL837 7-ETHYL-10-HYDROXYCAMPTOTHECIN IC50 = 80.0 nM 7.10
CHEMBL323751 IC50 = 100.0 nM 7.00
CHEMBL112769 IC50 = 130.0 nM 6.89
CHEMBL322337 IC50 = 130.0 nM 6.89
CHEMBL111209 IC50 = 140.0 nM 6.85
CHEMBL113482 IC50 = 160.0 nM 6.80
CHEMBL320127 IC50 = 200.0 nM 6.70
CHEMBL112334 IC50 = 210.0 nM 6.68
CHEMBL113558 IC50 = 280.0 nM 6.55
CHEMBL113393 IC50 = 300.0 nM 6.52
CHEMBL65 CAMPTOTHECIN IC50 = 330.0 nM 6.48
CHEMBL114135 IC50 = 340.0 nM 6.47
CHEMBL3215370 IC50 = 360.0 nM 6.44
CHEMBL419186 IC50 = 490.0 nM 6.31
CHEMBL322141 IC50 = 500.0 nM 6.30
CHEMBL84 TOPOTECAN IC50 = 1380.0 nM 5.86
CHEMBL321273 IC50 = 1700.0 nM 5.77
CHEMBL109556 IC50 = 1770.0 nM 5.75
CHEMBL109233 IC50 = 2330.0 nM 5.63
CHEMBL419035 IC50 = 2400.0 nM 5.62
CHEMBL109734 IC50 = 3000.0 nM 5.52
CHEMBL112757 IC50 = 5130.0 nM 5.29
CHEMBL322063 IC50 = 5200.0 nM 5.28
CHEMBL444535 IC50 = 32000.0 nM 4.50
CHEMBL324292 IC50 = 48000.0 nM 4.32