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Assay Detail

CHEMBL5168875

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Functional
Anticancer activity in human PC-3M cells expressing PTB/GFP fusion protein assessed as perinucleolar compartment disassembly and measured after 24 hrs by Hoechst 33342 staining based microscopic method
ChEMBL ↗
132
Total Activities
81
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

PC-3M (CHEMBL4296484) ↗
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery and Optimization of Pyrrolopyrimidine Derivatives as Selective Disruptors of the Perinucleolar Compartment, a Marker of Tumor Progression toward Metastasis.
Frankowski KJ, Patnaik S, Wang C, Southall N, Dutta D, De S, Li D, Dextras C, Lin YH, Bryant-Connah M, Davis D, Wang F, Wachsmuth LM, Shah P, Williams J, Kabir M, Zhu E, Baljinnyam B, Wang A, Xu X, Norton J, Ferrer M, Titus S, Simeonov A, Zheng W, Mathews Griner LA, Jadhav A, Aubé J, Henderson MJ, Rudloff U, Schoenen FJ, Huang S, Marugan JJ.
J Med Chem (2022) 65 : 8303 -8331
PubMed 35696646 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 132 5.55 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5173509 — — 2 6.80
CHEMBL5195802 — — 2 6.77
CHEMBL4594433 ML-246 1.0 2 6.75
CHEMBL65 CAMPTOTHECIN -1.0 1 6.72
CHEMBL5208507 — — 2 6.60
CHEMBL5193081 — — 2 6.52
CHEMBL5197046 — — 2 6.50
CHEMBL5180011 — — 2 6.47
CHEMBL5174316 — — 2 6.30
CHEMBL5196965 — — 2 6.20
CHEMBL1467655 — — 2 6.08
CHEMBL5204369 — — 2 6.08
CHEMBL5186412 — — 2 6.08
CHEMBL53463 DOXORUBICIN 4.0 1 6.07
CHEMBL5176589 — — 2 6.03
CHEMBL5187302 — — 2 6.02
CHEMBL5207530 — — 2 6.02
CHEMBL5174794 — — 2 6.02
CHEMBL5207915 — — 2 5.96
CHEMBL5171725 — — 2 5.93
CHEMBL5189410 — — 2 5.88
CHEMBL1451774 — — 2 5.73
CHEMBL5202131 — — 2 5.70
CHEMBL5189579 — — 2 5.70
CHEMBL5177488 — — 2 5.67
CHEMBL5190839 — — 2 5.56
CHEMBL5184402 — — 2 5.55
CHEMBL5177741 — — 2 5.53
CHEMBL5195113 — — 2 5.50
CHEMBL5187869 — — 2 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5173509 — IC50 = 158.49 nM 6.80
CHEMBL5173509 — IC50 = 160.0 nM 6.80
CHEMBL5195802 — IC50 = 170.0 nM 6.77
CHEMBL5195802 — IC50 = 173.78 nM 6.76
CHEMBL4594433 ML-246 IC50 = 177.83 nM 6.75
CHEMBL65 CAMPTOTHECIN IC50 = 190.0 nM 6.72
CHEMBL4594433 ML-246 IC50 = 200.0 nM 6.70
CHEMBL5208507 — IC50 = 251.19 nM 6.60
CHEMBL5208507 — IC50 = 250.0 nM 6.60
CHEMBL5193081 — IC50 = 302.0 nM 6.52
CHEMBL5193081 — IC50 = 300.0 nM 6.52
CHEMBL5197046 — IC50 = 316.23 nM 6.50
CHEMBL5197046 — IC50 = 320.0 nM 6.50
CHEMBL5180011 — IC50 = 338.84 nM 6.47
CHEMBL5180011 — IC50 = 340.0 nM 6.47
CHEMBL5174316 — IC50 = 501.19 nM 6.30
CHEMBL5174316 — IC50 = 510.0 nM 6.29
CHEMBL5196965 — IC50 = 630.96 nM 6.20
CHEMBL5196965 — IC50 = 640.0 nM 6.19
CHEMBL1467655 — IC50 = 831.76 nM 6.08
CHEMBL5186412 — IC50 = 830.0 nM 6.08
CHEMBL1467655 — IC50 = 830.0 nM 6.08
CHEMBL5204369 — IC50 = 830.0 nM 6.08
CHEMBL5186412 — IC50 = 831.76 nM 6.08
CHEMBL5204369 — IC50 = 831.76 nM 6.08
CHEMBL53463 DOXORUBICIN IC50 = 860.0 nM 6.07
CHEMBL5176589 — IC50 = 933.25 nM 6.03
CHEMBL5176589 — IC50 = 930.0 nM 6.03
CHEMBL5207530 — IC50 = 960.0 nM 6.02
CHEMBL5174794 — IC50 = 960.0 nM 6.02
CHEMBL5187302 — IC50 = 954.99 nM 6.02
CHEMBL5174794 — IC50 = 954.99 nM 6.02
CHEMBL5207915 — IC50 = 1090.0 nM 5.96
CHEMBL5207915 — IC50 = 1096.48 nM 5.96
CHEMBL5171725 — IC50 = 1174.9 nM 5.93
CHEMBL5171725 — IC50 = 1180.0 nM 5.93
CHEMBL5189410 — IC50 = 1318.26 nM 5.88
CHEMBL5189410 — IC50 = 1310.0 nM 5.88
CHEMBL1451774 — IC50 = 1880.0 nM 5.73
CHEMBL1451774 — IC50 = 1862.09 nM 5.73
CHEMBL5189579 — IC50 = 2000.0 nM 5.70
CHEMBL5202131 — IC50 = 2020.0 nM 5.70
CHEMBL5202131 — IC50 = 1995.26 nM 5.70
CHEMBL5189579 — IC50 = 1995.26 nM 5.70
CHEMBL5177488 — IC50 = 2137.96 nM 5.67
CHEMBL5177488 — IC50 = 2170.0 nM 5.66
CHEMBL5187302 — IC50 = 2720.0 nM 5.57
CHEMBL5190839 — IC50 = 2730.0 nM 5.56
CHEMBL5190839 — IC50 = 2754.23 nM 5.56
CHEMBL5184402 — IC50 = 2818.38 nM 5.55