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Assay Detail

CHEMBL4734029

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

Functional
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 1 — Organism
Curated By Autocuration

Target

MDA-MB-231 (CHEMBL400)
Type CELL-LINE
Organism Homo sapiens

Publication

Potent antiproliferative activity of bradykinin B2 receptor selective agonist FR-190997 and analogue structures thereof: A paradox resolved?
Rassias G,Leonardi S,Rigopoulou D,Vachlioti E,Afratis K,Piperigkou Z,Koutsakis C,Karamanos NK,Gavras H,Papaioannou D
Eur J Med Chem (2021) 210 : 112948 -112948
PubMed 33139111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 5.94 10.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4787094 1 10.23
CHEMBL325041 BORTEZOMIB 3.0 1 8.52
CHEMBL4759582 1 8.30
CHEMBL92 DOCETAXEL ANHYDROUS 4.0 1 8.00
CHEMBL388978 STAUROSPORINE 1 8.00
CHEMBL159 VINBLASTINE 4.0 1 7.62
CHEMBL99869 1 7.10
CHEMBL53463 DOXORUBICIN 4.0 1 7.00
CHEMBL417 EPIRUBICIN 4.0 1 6.82
CHEMBL4754189 1 6.37
CHEMBL4749497 1 6.11
CHEMBL413 SIROLIMUS 4.0 1 6.05
CHEMBL428647 PACLITAXEL 4.0 1 6.05
CHEMBL888 GEMCITABINE 4.0 1 5.68
CHEMBL4749244 1 5.23
CHEMBL4784225 1 5.16
CHEMBL554 LAPATINIB 4.0 1 4.97
CHEMBL189963 PALBOCICLIB 4.0 1 4.84
CHEMBL32749 FERULATE -1.0 1 4.82
CHEMBL38 TRETINOIN 4.0 1 4.80
CHEMBL130517 FR-173657 1 4.70
CHEMBL4750888 1 4.66
CHEMBL3545110 RIBOCICLIB 4.0 1 4.56
CHEMBL2396661 ALPELISIB 4.0 1 4.20
CHEMBL521686 OLAPARIB 4.0 1 4.20
CHEMBL185 FLUOROURACIL 4.0 1 4.18
CHEMBL83 TAMOXIFEN 4.0 1 4.16
CHEMBL4740222 1 4.07
CHEMBL88 CYCLOPHOSPHAMIDE ANHYDROUS 4.0 1 -
CHEMBL1358 FULVESTRANT 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4787094 IC50 = 0.0594 nM 10.23
CHEMBL325041 BORTEZOMIB IC50 = 3.0 nM 8.52
CHEMBL4759582 IC50 = 5.0 nM 8.30
CHEMBL92 DOCETAXEL ANHYDROUS IC50 = 10.0 nM 8.00
CHEMBL388978 STAUROSPORINE IC50 = 10.0 nM 8.00
CHEMBL159 VINBLASTINE IC50 = 24.0 nM 7.62
CHEMBL99869 IC50 = 80.0 nM 7.10
CHEMBL53463 DOXORUBICIN IC50 = 100.0 nM 7.00
CHEMBL417 EPIRUBICIN IC50 = 150.0 nM 6.82
CHEMBL4754189 IC50 = 430.0 nM 6.37
CHEMBL4749497 IC50 = 780.0 nM 6.11
CHEMBL413 SIROLIMUS IC50 = 900.0 nM 6.05
CHEMBL428647 PACLITAXEL IC50 = 900.0 nM 6.05
CHEMBL888 GEMCITABINE IC50 = 2100.0 nM 5.68
CHEMBL4749244 IC50 = 5900.0 nM 5.23
CHEMBL4784225 IC50 = 6970.0 nM 5.16
CHEMBL554 LAPATINIB IC50 = 10600.0 nM 4.97
CHEMBL189963 PALBOCICLIB IC50 = 14600.0 nM 4.84
CHEMBL32749 FERULATE IC50 = 15000.0 nM 4.82
CHEMBL38 TRETINOIN IC50 = 16000.0 nM 4.80
CHEMBL130517 FR-173657 IC50 = 20000.0 nM 4.70
CHEMBL4750888 IC50 = 22000.0 nM 4.66
CHEMBL3545110 RIBOCICLIB IC50 = 27300.0 nM 4.56
CHEMBL2396661 ALPELISIB IC50 = 62900.0 nM 4.20
CHEMBL521686 OLAPARIB IC50 = 62500.0 nM 4.20
CHEMBL185 FLUOROURACIL IC50 = 66600.0 nM 4.18
CHEMBL83 TAMOXIFEN IC50 = 69700.0 nM 4.16
CHEMBL4740222 IC50 = 86000.0 nM 4.07
CHEMBL88 CYCLOPHOSPHAMIDE ANHYDROUS IC50 = 195500.0 nM -
CHEMBL1358 FULVESTRANT IC50 = 196300.0 nM -
CHEMBL4760768 IC50 = 520000.0 nM -
CHEMBL4797511 IC50 = 200000.0 nM -
CHEMBL4747403 IC50 = 193000.0 nM -
CHEMBL4800357 IC50 = 650000.0 nM -
CHEMBL4744780 IC50 = 450000.0 nM -