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Assay Detail

CHEMBL4827355

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

Functional
Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay
ChEMBL ↗
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7
Confidence 1 — Organism
Curated By Autocuration

Target

MCF7 (CHEMBL387) ↗
Type CELL-LINE
Organism Homo sapiens

Publication

GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.
Liang J, Zbieg JR, Blake RA, Chang JH, Daly S, DiPasquale AG, Friedman LS, Gelzleichter T, Gill M, Giltnane JM, Goodacre S, Guan J, Hartman SJ, Ingalla ER, Kategaya L, Kiefer JR, Kleinheinz T, Labadie SS, Lai T, Li J, Liao J, Liu Z, Mody V, McLean N, Metcalfe C, Nannini MA, Oeh J, O'Rourke MG, Ortwine DF, Ran Y, Ray NC, Roussel F, Sambrone A, Sampath D, Schutt LK, Vinogradova M, Wai J, Wang T, Wertz IE, White JR, Yeap SK, Young A, Zhang B, Zheng X, Zhou W, Zhong Y, Wang X.
J Med Chem (2021) 64 : 11841 -11856
PubMed 34251202 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 42 8.98 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4854930 — — 1 9.70
CHEMBL4447340 — — 1 9.52
CHEMBL4874160 — — 1 9.52
CHEMBL4845680 — — 1 9.52
CHEMBL4650316 GIREDESTRANT 3.0 1 9.40
CHEMBL4867106 — — 1 9.40
CHEMBL4857736 — — 1 9.30
CHEMBL4866043 — — 1 9.30
CHEMBL4877338 — — 1 9.30
CHEMBL4847664 — — 1 9.30
CHEMBL4862431 — — 1 9.22
CHEMBL4871161 — — 1 9.22
CHEMBL4866232 — — 1 9.22
CHEMBL4856892 — — 1 9.22
CHEMBL4864829 — — 1 9.22
CHEMBL4862453 — — 1 9.22
CHEMBL4858543 — — 1 9.15
CHEMBL4845726 — — 1 9.15
CHEMBL4649161 — — 1 9.15
CHEMBL4869698 — — 1 9.10
CHEMBL4756497 — — 1 9.10
CHEMBL4852984 — — 1 9.05
CHEMBL4868243 — — 1 9.05
CHEMBL4847707 — — 1 9.00
CHEMBL4873860 — — 1 9.00
CHEMBL4528514 — — 1 9.00
CHEMBL4871601 — — 1 8.96
CHEMBL4850919 — — 1 8.92
CHEMBL4853118 — — 1 8.85
CHEMBL4856969 — — 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4854930 — EC50 = 0.2 nM 9.70
CHEMBL4447340 — EC50 = 0.3 nM 9.52
CHEMBL4845680 — EC50 = 0.3 nM 9.52
CHEMBL4874160 — EC50 = 0.3 nM 9.52
CHEMBL4650316 GIREDESTRANT EC50 = 0.4 nM 9.40
CHEMBL4867106 — EC50 = 0.4 nM 9.40
CHEMBL4857736 — EC50 = 0.5 nM 9.30
CHEMBL4866043 — EC50 = 0.5 nM 9.30
CHEMBL4877338 — EC50 = 0.5 nM 9.30
CHEMBL4847664 — EC50 = 0.5 nM 9.30
CHEMBL4862453 — EC50 = 0.6 nM 9.22
CHEMBL4862431 — EC50 = 0.6 nM 9.22
CHEMBL4871161 — EC50 = 0.6 nM 9.22
CHEMBL4866232 — EC50 = 0.6 nM 9.22
CHEMBL4856892 — EC50 = 0.6 nM 9.22
CHEMBL4864829 — EC50 = 0.6 nM 9.22
CHEMBL4858543 — EC50 = 0.7 nM 9.15
CHEMBL4845726 — EC50 = 0.7 nM 9.15
CHEMBL4649161 — EC50 = 0.7 nM 9.15
CHEMBL4869698 — EC50 = 0.8 nM 9.10
CHEMBL4756497 — EC50 = 0.8 nM 9.10
CHEMBL4852984 — EC50 = 0.9 nM 9.05
CHEMBL4868243 — EC50 = 0.9 nM 9.05
CHEMBL4847707 — EC50 = 1.0 nM 9.00
CHEMBL4873860 — EC50 = 1.0 nM 9.00
CHEMBL4528514 — EC50 = 1.0 nM 9.00
CHEMBL4871601 — EC50 = 1.1 nM 8.96
CHEMBL4850919 — EC50 = 1.2 nM 8.92
CHEMBL4853118 — EC50 = 1.4 nM 8.85
CHEMBL4856969 — EC50 = 1.4 nM 8.85
CHEMBL4860671 — EC50 = 2.1 nM 8.68
CHEMBL1358 FULVESTRANT EC50 = 2.4 nM 8.62
CHEMBL4865515 — EC50 = 2.7 nM 8.57
CHEMBL4854999 — EC50 = 2.8 nM 8.55
CHEMBL4877406 — EC50 = 2.8 nM 8.55
CHEMBL489 AFIMOXIFENE EC50 = 3.5 nM 8.46
CHEMBL4864628 — EC50 = 9.8 nM 8.01
CHEMBL4869612 — EC50 = 10.0 nM 8.00
CHEMBL4864337 — EC50 = 11.0 nM 7.96
CHEMBL3581693 BRILANESTRANT EC50 = 17.0 nM 7.77
CHEMBL4877353 — EC50 > 200.0 nM -
CHEMBL83 TAMOXIFEN EC50 > 200.0 nM -