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Assay Detail

CHEMBL4827352

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Binding
Antagonist activity at estrogen receptor in human T47D cells incubated for 18 hrs by ultra high sensitivity luminescence reporter gene assay
ChEMBL ↗
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type T47D
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor (CHEMBL206) ↗
Type SINGLE PROTEIN
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
IC50 42 9.39 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4650316 GIREDESTRANT 3.0 1 10.30
CHEMBL4866043 — — 1 10.22
CHEMBL4856969 — — 1 10.15
CHEMBL4856892 — — 1 10.10
CHEMBL4845726 — — 1 10.05
CHEMBL4869698 — — 1 10.05
CHEMBL4864829 — — 1 10.05
CHEMBL4447340 — — 1 10.00
CHEMBL4871161 — — 1 10.00
CHEMBL4857736 — — 1 9.89
CHEMBL4649161 — — 1 9.85
CHEMBL4877338 — — 1 9.82
CHEMBL4853118 — — 1 9.80
CHEMBL4860671 — — 1 9.80
CHEMBL4756497 — — 1 9.70
CHEMBL4866232 — — 1 9.64
CHEMBL1358 FULVESTRANT 4.0 1 9.60
CHEMBL4873860 — — 1 9.60
CHEMBL4871601 — — 1 9.54
CHEMBL4847707 — — 1 9.52
CHEMBL4854930 — — 1 9.40
CHEMBL4850919 — — 1 9.40
CHEMBL4867106 — — 1 9.30
CHEMBL4528514 — — 1 9.28
CHEMBL4877406 — — 1 9.22
CHEMBL4852984 — — 1 9.15
CHEMBL4847664 — — 1 9.10
CHEMBL4858543 — — 1 9.10
CHEMBL4864337 — — 1 9.05
CHEMBL4865515 — — 1 9.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4650316 GIREDESTRANT IC50 = 0.05 nM 10.30
CHEMBL4866043 — IC50 = 0.06 nM 10.22
CHEMBL4856969 — IC50 = 0.07 nM 10.15
CHEMBL4856892 — IC50 = 0.08 nM 10.10
CHEMBL4845726 — IC50 = 0.09 nM 10.05
CHEMBL4869698 — IC50 = 0.09 nM 10.05
CHEMBL4864829 — IC50 = 0.09 nM 10.05
CHEMBL4447340 — IC50 = 0.1 nM 10.00
CHEMBL4871161 — IC50 = 0.1 nM 10.00
CHEMBL4857736 — IC50 = 0.13 nM 9.89
CHEMBL4649161 — IC50 = 0.14 nM 9.85
CHEMBL4877338 — IC50 = 0.15 nM 9.82
CHEMBL4853118 — IC50 = 0.16 nM 9.80
CHEMBL4860671 — IC50 = 0.16 nM 9.80
CHEMBL4756497 — IC50 = 0.2 nM 9.70
CHEMBL4866232 — IC50 = 0.23 nM 9.64
CHEMBL1358 FULVESTRANT IC50 = 0.25 nM 9.60
CHEMBL4873860 — IC50 = 0.25 nM 9.60
CHEMBL4871601 — IC50 = 0.29 nM 9.54
CHEMBL4847707 — IC50 = 0.3 nM 9.52
CHEMBL4850919 — IC50 = 0.4 nM 9.40
CHEMBL4854930 — IC50 = 0.4 nM 9.40
CHEMBL4867106 — IC50 = 0.5 nM 9.30
CHEMBL4528514 — IC50 = 0.53 nM 9.28
CHEMBL4877406 — IC50 = 0.6 nM 9.22
CHEMBL4852984 — IC50 = 0.7 nM 9.15
CHEMBL4847664 — IC50 = 0.8 nM 9.10
CHEMBL4858543 — IC50 = 0.8 nM 9.10
CHEMBL4864337 — IC50 = 0.89 nM 9.05
CHEMBL4865515 — IC50 = 0.98 nM 9.01
CHEMBL489 AFIMOXIFENE IC50 = 1.36 nM 8.87
CHEMBL4864628 — IC50 = 2.1 nM 8.68
CHEMBL4854999 — IC50 = 3.6 nM 8.44
CHEMBL3581693 BRILANESTRANT IC50 = 5.31 nM 8.28
CHEMBL4862431 — IC50 = 6.0 nM 8.22
CHEMBL4869612 — IC50 = 12.0 nM 7.92
CHEMBL83 TAMOXIFEN IC50 = 58.0 nM 7.24
CHEMBL4874160 — IC50 - — -
CHEMBL4845680 — IC50 - — -
CHEMBL4862453 — IC50 - — -
CHEMBL4868243 — IC50 - — -
CHEMBL4877353 — IC50 > 1000.0 nM -