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Assay Detail

CHEMBL972520

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

Functional
Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay
ChEMBL ↗
38
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KB 3-1
Confidence 1 — Organism
Curated By Autocuration

Target

NON-PROTEIN TARGET (CHEMBL3879801) ↗
Type NON-MOLECULAR

Publication

Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.
Hall MD, Salam NK, Hellawell JL, Fales HM, Kensler CB, Ludwig JA, Szakács G, Hibbs DE, Gottesman MM.
J Med Chem (2009) 52 : 3191 -3204
PubMed 19397322 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 4.97 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL231616 TRIAPINE 3.0 2 5.85
CHEMBL443772 — — 2 5.72
CHEMBL535 SUNITINIB 4.0 1 5.64
CHEMBL470509 — — 2 5.47
CHEMBL474400 — — 2 5.36
CHEMBL495479 — — 2 4.88
CHEMBL504574 — — 2 4.85
CHEMBL376584 — — 2 4.84
CHEMBL390341 — — 2 4.77
CHEMBL474417 — — 2 4.71
CHEMBL523326 — — 2 4.58
CHEMBL489742 — — 2 4.58
CHEMBL489938 — — 1 4.56
CHEMBL492408 — — 2 4.55
CHEMBL474416 — — 2 4.41
CHEMBL523111 — — 1 -
CHEMBL333137 — — 1 -
CHEMBL514013 — — 1 -
CHEMBL444521 — — 1 -
CHEMBL525231 — — 1 -
CHEMBL491979 — — 1 -
CHEMBL491309 — — 1 -
CHEMBL375492 AMITHIOZONE 2.0 1 -
CHEMBL326294 ISATIN — 1 -
CHEMBL493237 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL231616 TRIAPINE IC50 = 1400.0 nM 5.85
CHEMBL231616 TRIAPINE IC50 = 1412.54 nM 5.85
CHEMBL443772 — IC50 = 1900.0 nM 5.72
CHEMBL443772 — IC50 = 1905.46 nM 5.72
CHEMBL535 SUNITINIB IC50 = 2300.0 nM 5.64
CHEMBL470509 — IC50 = 3388.44 nM 5.47
CHEMBL470509 — IC50 = 3400.0 nM 5.47
CHEMBL474400 — IC50 = 4400.0 nM 5.36
CHEMBL474400 — IC50 = 4365.16 nM 5.36
CHEMBL495479 — IC50 = 13100.0 nM 4.88
CHEMBL495479 — IC50 = 13182.57 nM 4.88
CHEMBL504574 — IC50 = 14200.0 nM 4.85
CHEMBL504574 — IC50 = 14125.38 nM 4.85
CHEMBL376584 — IC50 = 14500.0 nM 4.84
CHEMBL376584 — IC50 = 14454.4 nM 4.84
CHEMBL390341 — IC50 = 17000.0 nM 4.77
CHEMBL474417 — IC50 = 19498.45 nM 4.71
CHEMBL474417 — IC50 = 19600.0 nM 4.71
CHEMBL489742 — IC50 = 26302.68 nM 4.58
CHEMBL523326 — IC50 = 26302.68 nM 4.58
CHEMBL523326 — IC50 = 26100.0 nM 4.58
CHEMBL489742 — IC50 = 26300.0 nM 4.58
CHEMBL489938 — IC50 = 27700.0 nM 4.56
CHEMBL390341 — IC50 = 28183.83 nM 4.55
CHEMBL492408 — IC50 = 28183.83 nM 4.55
CHEMBL492408 — IC50 = 28400.0 nM 4.55
CHEMBL474416 — IC50 = 38904.51 nM 4.41
CHEMBL474416 — IC50 = 39300.0 nM 4.41
CHEMBL491309 — IC50 > 50000.0 nM -
CHEMBL491979 — IC50 > 50000.0 nM -
CHEMBL333137 — IC50 > 50000.0 nM -
CHEMBL525231 — IC50 > 50000.0 nM -
CHEMBL444521 — IC50 > 50000.0 nM -
CHEMBL514013 — IC50 > 50000.0 nM -
CHEMBL326294 ISATIN IC50 > 50000.0 nM -
CHEMBL375492 AMITHIOZONE IC50 > 50000.0 nM -
CHEMBL493237 — IC50 > 50000.0 nM -
CHEMBL523111 — IC50 > 50000.0 nM -