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Assay Detail

CHEMBL5241250

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Binding
Inhibition of aromatase (unknown origin)
ChEMBL ↗
140
Total Activities
138
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aromatase (CHEMBL1978) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Effective anti-aromatase therapy to battle against estrogen-mediated breast cancer: Comparative SAR/QSAR assessment on steroidal aromatase inhibitors.
Adhikari N, Baidya SK, Jha T.
Eur J Med Chem (2020) 208 : 112845 -112845
PubMed 33017749 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 140 5.89 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3753447 — — 1 8.11
CHEMBL5286289 — — 1 8.00
CHEMBL3753373 — — 1 7.89
CHEMBL3752221 — — 1 7.83
CHEMBL3754259 — — 1 7.78
CHEMBL3754055 — — 1 7.73
CHEMBL3754204 — — 1 7.21
CHEMBL5280059 — — 1 7.07
CHEMBL3752998 — — 1 7.06
CHEMBL3753169 — — 1 7.05
CHEMBL5290133 — — 1 7.02
CHEMBL5268139 — — 1 7.00
CHEMBL5270074 — — 1 6.85
CHEMBL5272287 — — 1 6.82
CHEMBL5267234 — — 1 6.82
CHEMBL3623214 — — 1 6.80
CHEMBL5269898 — — 1 6.77
CHEMBL3754054 — — 1 6.76
CHEMBL3623213 — — 1 6.75
CHEMBL5273888 — — 1 6.70
CHEMBL5278342 — — 1 6.68
CHEMBL5286772 — — 1 6.68
CHEMBL3752591 — — 1 6.63
CHEMBL3752414 — — 2 6.60
CHEMBL3753403 — — 1 6.60
CHEMBL5290788 — — 2 6.55
CHEMBL5266491 — — 1 6.46
CHEMBL132530 FORMESTANE 2.0 1 6.43
CHEMBL5291406 — — 1 6.38
CHEMBL5289646 — — 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3753447 — IC50 = 7.691 nM 8.11
CHEMBL5286289 — IC50 = 9.908 nM 8.00
CHEMBL3753373 — IC50 = 12.91 nM 7.89
CHEMBL3752221 — IC50 = 14.89 nM 7.83
CHEMBL3754259 — IC50 = 16.71 nM 7.78
CHEMBL3754055 — IC50 = 18.71 nM 7.73
CHEMBL3754204 — IC50 = 60.95 nM 7.21
CHEMBL5280059 — IC50 = 84.92 nM 7.07
CHEMBL3752998 — IC50 = 87.9 nM 7.06
CHEMBL3753169 — IC50 = 88.92 nM 7.05
CHEMBL5290133 — IC50 = 95.06 nM 7.02
CHEMBL5268139 — IC50 = 100.0 nM 7.00
CHEMBL5270074 — IC50 = 139.96 nM 6.85
CHEMBL5272287 — IC50 = 149.97 nM 6.82
CHEMBL5267234 — IC50 = 149.97 nM 6.82
CHEMBL3623214 — IC50 = 159.96 nM 6.80
CHEMBL5269898 — IC50 = 169.82 nM 6.77
CHEMBL3754054 — IC50 = 172.19 nM 6.76
CHEMBL3623213 — IC50 = 179.89 nM 6.75
CHEMBL5273888 — IC50 = 199.99 nM 6.70
CHEMBL5286772 — IC50 = 209.89 nM 6.68
CHEMBL5278342 — IC50 = 209.89 nM 6.68
CHEMBL3752591 — IC50 = 231.74 nM 6.63
CHEMBL3752414 — IC50 = 250.03 nM 6.60
CHEMBL3753403 — IC50 = 250.03 nM 6.60
CHEMBL5290788 — IC50 = 279.9 nM 6.55
CHEMBL5266491 — IC50 = 349.95 nM 6.46
CHEMBL132530 FORMESTANE IC50 = 369.83 nM 6.43
CHEMBL5291406 — IC50 = 419.76 nM 6.38
CHEMBL5289646 — IC50 = 439.54 nM 6.36
CHEMBL5283868 — IC50 = 460.26 nM 6.34
CHEMBL3752414 — IC50 = 460.26 nM 6.34
CHEMBL3623219 — IC50 = 479.73 nM 6.32
CHEMBL5290960 — IC50 = 489.78 nM 6.31
CHEMBL5270764 — IC50 = 500.03 nM 6.30
CHEMBL5289279 — IC50 = 529.66 nM 6.28
CHEMBL5275417 — IC50 = 529.66 nM 6.28
CHEMBL5275053 — IC50 = 539.51 nM 6.27
CHEMBL3753307 — IC50 = 549.54 nM 6.26
CHEMBL5279458 — IC50 = 549.54 nM 6.26
CHEMBL2179108 — IC50 = 559.76 nM 6.25
CHEMBL3754505 — IC50 = 599.79 nM 6.22
CHEMBL5270517 — IC50 = 599.79 nM 6.22
CHEMBL2179107 — IC50 = 619.44 nM 6.21
CHEMBL3753089 — IC50 = 660.69 nM 6.18
CHEMBL5276194 — IC50 = 660.69 nM 6.18
CHEMBL5279329 — IC50 = 699.84 nM 6.16
CHEMBL5268850 — IC50 = 749.89 nM 6.12
CHEMBL5290320 — IC50 = 779.83 nM 6.11
CHEMBL5270578 — IC50 = 799.83 nM 6.10