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

CHEMBL5121196

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

Binding
Antagonist activity at ERalpha (unknown origin)
ChEMBL ↗
38
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Estrogen receptor (CHEMBL206) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Human estrogen receptor α antagonists, part 2: Synthesis driven by rational design, in vitro antiproliferative, and in vivo anticancer evaluation of innovative coumarin-related antiestrogens as breast cancer suppressants.
Kurtanović N, Tomašević N, Matić S, Mitrović MM, Kostić DA, Sabatino M, Antonini L, Ragno R, Mladenović M.
Eur J Med Chem (2022) 227 : 113869 -113869
PubMed 34710747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.50 9.72
Ka 19 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5199803 — — 2 9.72
CHEMBL5184399 — — 2 9.59
CHEMBL5178058 — — 2 9.48
CHEMBL5195371 — — 2 9.41
CHEMBL5191405 — — 2 9.17
CHEMBL5174813 — — 2 9.15
CHEMBL81 RALOXIFENE 4.0 2 9.13
CHEMBL5187253 — — 2 9.12
CHEMBL5207726 — — 2 9.12
CHEMBL135 ESTRADIOL 4.0 2 9.05
CHEMBL5203282 — — 2 8.98
CHEMBL5178110 — — 2 8.95
CHEMBL489 AFIMOXIFENE 3.0 2 8.95
CHEMBL5181808 — — 2 7.43
CHEMBL5187730 — — 2 7.41
CHEMBL5198828 — — 2 6.84
CHEMBL5209099 — — 2 6.79
CHEMBL5194045 — — 2 6.77
CHEMBL5196340 — — 2 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5199803 — IC50 = 0.19 nM 9.72
CHEMBL5184399 — IC50 = 0.26 nM 9.59
CHEMBL5178058 — IC50 = 0.33 nM 9.48
CHEMBL5195371 — IC50 = 0.39 nM 9.41
CHEMBL5191405 — IC50 = 0.67 nM 9.17
CHEMBL5174813 — IC50 = 0.71 nM 9.15
CHEMBL81 RALOXIFENE IC50 = 0.74 nM 9.13
CHEMBL5187253 — IC50 = 0.76 nM 9.12
CHEMBL5207726 — IC50 = 0.75 nM 9.12
CHEMBL135 ESTRADIOL IC50 = 0.89 nM 9.05
CHEMBL5203282 — IC50 = 1.05 nM 8.98
CHEMBL5178110 — IC50 = 1.13 nM 8.95
CHEMBL489 AFIMOXIFENE IC50 = 1.12 nM 8.95
CHEMBL5181808 — IC50 = 37.0 nM 7.43
CHEMBL5187730 — IC50 = 39.0 nM 7.41
CHEMBL5198828 — IC50 = 143.93 nM 6.84
CHEMBL5209099 — IC50 = 160.53 nM 6.79
CHEMBL5194045 — IC50 = 168.41 nM 6.77
CHEMBL5196340 — IC50 = 375.32 nM 6.43
CHEMBL5178058 — Ka = 0.07 nM -
CHEMBL5209099 — Ka = 36.07 nM -
CHEMBL5184399 — Ka = 0.06 nM -
CHEMBL5198828 — Ka = 32.34 nM -
CHEMBL5187253 — Ka = 0.17 nM -
CHEMBL5196340 — Ka = 84.34 nM -
CHEMBL5199803 — Ka = 0.04 nM -
CHEMBL5181808 — Ka = 0.04 nM -
CHEMBL5187730 — Ka = 0.08 nM -
CHEMBL5195371 — Ka = 0.08 nM -
CHEMBL5174813 — Ka = 0.16 nM -
CHEMBL5207726 — Ka = 0.17 nM -
CHEMBL5203282 — Ka = 0.24 nM -
CHEMBL5178110 — Ka = 0.25 nM -
CHEMBL5191405 — Ka = 0.15 nM -
CHEMBL5194045 — Ka = 37.84 nM -
CHEMBL135 ESTRADIOL Ka = 0.2 nM -
CHEMBL489 AFIMOXIFENE Ka = 0.25 nM -
CHEMBL81 RALOXIFENE Ka = 0.17 nM -