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Assay Detail

CHEMBL826376

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

Binding
Displacement of [3H]DHT from androgen receptor of human MDA-453 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-453
Confidence 9 — Direct single protein target
Curated By Expert

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.
Balog A, Salvati ME, Shan W, Mathur A, Leith LW, Wei DD, Attar RM, Geng J, Rizzo CA, Wang C, Krystek SR, Tokarski JS, Hunt JT, Gottardis M, Weinmann R.
Bioorg Med Chem Lett (2004) 14 : 6107 -6111
PubMed 15546739 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.17 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL185880 1 9.00
CHEMBL188297 1 8.30
CHEMBL365650 1 8.00
CHEMBL426623 1 8.00
CHEMBL362566 1 8.00
CHEMBL187605 1 7.40
CHEMBL365921 1 7.40
CHEMBL188129 1 7.22
CHEMBL409 BICALUTAMIDE 4.0 1 7.19
CHEMBL365482 1 7.16
CHEMBL371392 1 7.00
CHEMBL189600 1 6.92
CHEMBL414845 1 6.75
CHEMBL188857 1 6.72
CHEMBL364393 1 6.64
CHEMBL188803 1 6.62
CHEMBL447184 1 6.16
CHEMBL188545 1 5.99
CHEMBL188261 1 5.85
CHEMBL188681 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL185880 Ki = 1.0 nM 9.00
CHEMBL188297 Ki = 5.0 nM 8.30
CHEMBL365650 Ki = 10.0 nM 8.00
CHEMBL426623 Ki = 10.0 nM 8.00
CHEMBL362566 Ki = 10.0 nM 8.00
CHEMBL187605 Ki = 40.0 nM 7.40
CHEMBL365921 Ki = 40.0 nM 7.40
CHEMBL188129 Ki = 60.0 nM 7.22
CHEMBL409 BICALUTAMIDE Ki = 65.0 nM 7.19
CHEMBL365482 Ki = 70.0 nM 7.16
CHEMBL371392 Ki = 100.0 nM 7.00
CHEMBL189600 Ki = 120.0 nM 6.92
CHEMBL414845 Ki = 180.0 nM 6.75
CHEMBL188857 Ki = 190.0 nM 6.72
CHEMBL364393 Ki = 230.0 nM 6.64
CHEMBL188803 Ki = 240.0 nM 6.62
CHEMBL447184 Ki = 690.0 nM 6.16
CHEMBL188545 Ki = 1030.0 nM 5.99
CHEMBL188261 Ki = 1400.0 nM 5.85
CHEMBL188681 Ki > 5000.0 nM -