Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5326436

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

ADMET
Inhibition of human recombinant aromatase using ARO as substrate
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aromatase (CHEMBL1978) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-guided identification of novel dual-targeting estrogen receptor α degraders with aromatase inhibitory activity for the treatment of endocrine-resistant breast cancer.
Xin L, Min J, Hu H, Li Y, Du C, Xie B, Cheng Y, Deng X, Deng X, Shen K, Huang J, Chen CC, Guo RT, Dong C, Zhou HB.
Eur J Med Chem (2023) 253 : 115328 -115328
PubMed 37037140 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 7.28 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5433442 — — 1 9.05
CHEMBL5412790 — — 1 8.89
CHEMBL1444 LETROZOLE 4.0 1 8.74
CHEMBL5405944 — — 1 8.68
CHEMBL5421409 — — 1 8.46
CHEMBL5411799 — — 1 8.37
CHEMBL5408038 — — 1 8.11
CHEMBL5400803 — — 1 7.81
CHEMBL5417452 — — 1 7.69
CHEMBL5423258 — — 1 7.66
CHEMBL5400203 — — 1 7.58
CHEMBL5426947 — — 1 7.49
CHEMBL5404063 — — 1 7.42
CHEMBL5422315 — — 1 7.26
CHEMBL5394007 — — 1 7.05
CHEMBL5426175 — — 1 7.00
CHEMBL5428681 — — 1 7.00
CHEMBL5436925 — — 1 6.99
CHEMBL5401146 — — 1 6.96
CHEMBL5435743 — — 1 6.89
CHEMBL5427513 — — 1 6.84
CHEMBL5414572 — — 1 6.82
CHEMBL5407335 — — 1 6.81
CHEMBL5402392 — — 1 6.71
CHEMBL5413340 — — 1 6.63
CHEMBL5403786 — — 1 6.57
CHEMBL5404699 — — 1 6.55
CHEMBL5426251 — — 1 6.54
CHEMBL5418690 — — 1 6.49
CHEMBL5410004 — — 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5433442 — IC50 = 0.9 nM 9.05
CHEMBL5412790 — IC50 = 1.3 nM 8.89
CHEMBL1444 LETROZOLE IC50 = 1.8 nM 8.74
CHEMBL5405944 — IC50 = 2.09 nM 8.68
CHEMBL5421409 — IC50 = 3.48 nM 8.46
CHEMBL5411799 — IC50 = 4.3 nM 8.37
CHEMBL5408038 — IC50 = 7.8 nM 8.11
CHEMBL5400803 — IC50 = 15.46 nM 7.81
CHEMBL5417452 — IC50 = 20.42 nM 7.69
CHEMBL5423258 — IC50 = 21.8 nM 7.66
CHEMBL5400203 — IC50 = 26.52 nM 7.58
CHEMBL5426947 — IC50 = 32.3 nM 7.49
CHEMBL5404063 — IC50 = 37.73 nM 7.42
CHEMBL5422315 — IC50 = 54.83 nM 7.26
CHEMBL5394007 — IC50 = 89.8 nM 7.05
CHEMBL5426175 — IC50 = 101.0 nM 7.00
CHEMBL5428681 — IC50 = 101.12 nM 7.00
CHEMBL5436925 — IC50 = 103.24 nM 6.99
CHEMBL5401146 — IC50 = 110.08 nM 6.96
CHEMBL5435743 — IC50 = 127.4 nM 6.89
CHEMBL5427513 — IC50 = 144.58 nM 6.84
CHEMBL5414572 — IC50 = 152.12 nM 6.82
CHEMBL5407335 — IC50 = 154.7 nM 6.81
CHEMBL5402392 — IC50 = 197.0 nM 6.71
CHEMBL5413340 — IC50 = 236.72 nM 6.63
CHEMBL5403786 — IC50 = 267.25 nM 6.57
CHEMBL5404699 — IC50 = 282.0 nM 6.55
CHEMBL5426251 — IC50 = 286.42 nM 6.54
CHEMBL5418690 — IC50 = 323.0 nM 6.49
CHEMBL5410004 — IC50 = 329.2 nM 6.48
CHEMBL5433532 — IC50 = 376.2 nM 6.42
CHEMBL5423781 — IC50 = 543.62 nM 6.26
CHEMBL5420394 — IC50 = 877.4 nM 6.06
CHEMBL5399056 — IC50 - — -
CHEMBL4800654 — IC50 - — -
CHEMBL489 AFIMOXIFENE IC50 - — -
CHEMBL5403080 — IC50 - — -
CHEMBL5424929 — IC50 - — -
CHEMBL5436713 — IC50 - — -
CHEMBL5419649 — IC50 - — -
CHEMBL5414261 — IC50 - — -
CHEMBL5414659 — IC50 - — -
CHEMBL5396802 — IC50 - — -
CHEMBL1358 FULVESTRANT IC50 - — -
CHEMBL5398866 — IC50 - — -
CHEMBL5432102 — IC50 - — -
CHEMBL5394879 — IC50 - — -
CHEMBL5423408 — IC50 - — -
CHEMBL5398724 — IC50 - — -
CHEMBL5394546 — IC50 - — -