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Assay Detail

CHEMBL1052829

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Functional
Antiproliferative activity against human BT474 cells after 72 hrs by MTT assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type BT-474
Confidence 1 — Organism
Curated By Autocuration

Target

BT-474 (CHEMBL614529)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.
Gavai AV, Fink BE, Fairfax DJ, Martin GS, Rossiter LM, Holst CL, Kim SH, Leavitt KJ, Mastalerz H, Han WC, Norris D, Goyal B, Swaminathan S, Patel B, Mathur A, Vyas DM, Tokarski JS, Yu C, Oppenheimer S, Zhang H, Marathe P, Fargnoli J, Lee FY, Wong TW, Vite GD.
J Med Chem (2009) 52 : 6527 -6530
PubMed 19821562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.60 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL565714 1 7.15
CHEMBL583218 1 7.05
CHEMBL567197 1 6.89
CHEMBL578044 1 6.89
CHEMBL583403 1 6.72
CHEMBL565467 1 6.54
CHEMBL566350 1 6.51
CHEMBL584714 1 6.51
CHEMBL1645462 AC-480 1.0 1 6.51
CHEMBL567873 1 6.38
CHEMBL566559 1 6.33
CHEMBL578255 1 6.26
CHEMBL566337 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL565714 IC50 = 71.0 nM 7.15
CHEMBL583218 IC50 = 90.0 nM 7.05
CHEMBL567197 IC50 = 130.0 nM 6.89
CHEMBL578044 IC50 = 130.0 nM 6.89
CHEMBL583403 IC50 = 190.0 nM 6.72
CHEMBL565467 IC50 = 290.0 nM 6.54
CHEMBL566350 IC50 = 310.0 nM 6.51
CHEMBL584714 IC50 = 310.0 nM 6.51
CHEMBL1645462 AC-480 IC50 = 310.0 nM 6.51
CHEMBL567873 IC50 = 420.0 nM 6.38
CHEMBL566559 IC50 = 470.0 nM 6.33
CHEMBL578255 IC50 = 550.0 nM 6.26
CHEMBL566337 IC50 = 860.0 nM 6.07