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Assay Detail

CHEMBL5121197

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

Binding
Antagonist activity at ERbeta (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 beta (CHEMBL242) ↗
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 7.16 9.05
Ka 19 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 2 9.05
CHEMBL489 AFIMOXIFENE 3.0 2 8.44
CHEMBL5209099 — — 2 7.54
CHEMBL5194045 — — 2 7.50
CHEMBL5196340 — — 2 7.43
CHEMBL5174813 — — 2 7.37
CHEMBL5198828 — — 2 7.34
CHEMBL5178110 — — 2 7.21
CHEMBL5191405 — — 2 7.17
CHEMBL5203282 — — 2 7.16
CHEMBL5181808 — — 2 7.14
CHEMBL5187730 — — 2 7.13
CHEMBL5178058 — — 2 7.11
CHEMBL5195371 — — 2 7.10
CHEMBL5187253 — — 2 7.06
CHEMBL5184399 — — 2 7.01
CHEMBL5199803 — — 2 6.99
CHEMBL5207726 — — 2 5.24
CHEMBL81 RALOXIFENE 4.0 2 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL IC50 = 0.89 nM 9.05
CHEMBL489 AFIMOXIFENE IC50 = 3.61 nM 8.44
CHEMBL5209099 — IC50 = 28.82 nM 7.54
CHEMBL5194045 — IC50 = 31.87 nM 7.50
CHEMBL5196340 — IC50 = 36.78 nM 7.43
CHEMBL5174813 — IC50 = 42.73 nM 7.37
CHEMBL5198828 — IC50 = 45.43 nM 7.34
CHEMBL5178110 — IC50 = 62.09 nM 7.21
CHEMBL5191405 — IC50 = 67.14 nM 7.17
CHEMBL5203282 — IC50 = 69.88 nM 7.16
CHEMBL5181808 — IC50 = 72.48 nM 7.14
CHEMBL5187730 — IC50 = 74.46 nM 7.13
CHEMBL5178058 — IC50 = 77.53 nM 7.11
CHEMBL5195371 — IC50 = 79.54 nM 7.10
CHEMBL5187253 — IC50 = 86.41 nM 7.06
CHEMBL5184399 — IC50 = 98.25 nM 7.01
CHEMBL5199803 — IC50 = 102.47 nM 6.99
CHEMBL5207726 — IC50 = 5732.0 nM 5.24
CHEMBL81 RALOXIFENE IC50 = 7430.0 nM 5.13
CHEMBL5178058 — Ka = 43.56 nM -
CHEMBL5209099 — Ka = 16.19 nM -
CHEMBL5184399 — Ka = 55.2 nM -
CHEMBL5198828 — Ka = 25.52 nM -
CHEMBL5187253 — Ka = 48.54 nM -
CHEMBL5196340 — Ka = 20.66 nM -
CHEMBL5199803 — Ka = 57.57 nM -
CHEMBL5181808 — Ka = 40.72 nM -
CHEMBL5187730 — Ka = 41.83 nM -
CHEMBL5195371 — Ka = 44.69 nM -
CHEMBL5174813 — Ka = 24.01 nM -
CHEMBL5207726 — Ka = 32.2 nM -
CHEMBL5203282 — Ka = 39.26 nM -
CHEMBL5178110 — Ka = 34.88 nM -
CHEMBL5191405 — Ka = 37.72 nM -
CHEMBL5194045 — Ka = 17.9 nM -
CHEMBL135 ESTRADIOL Ka = 0.5 nM -
CHEMBL489 AFIMOXIFENE Ka = 2.03 nM -
CHEMBL81 RALOXIFENE Ka = 41.24 nM -