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Drug-Target Interaction

Drug

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PubChem ID:4713
Structure:
Synonyms:
"2′-amino-3′-methoxyflavone"
167869-21-8
2′-Amino-3′-methoxyflavone
2'-AMINO-3'-METHOXYFLAVONE
2-(2'-amino-3'-methoxyphenyl)oxanaphthalen-4-one
2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one
2-(2-Amino-3-methoxyphenyl)-chromen-4-one
2-(2-amino-3-methoxyphenyl)chromen-4-one
4H-1-Benzopyran-4-one, 2-(2-amino-3-methoxyphenyl)-
4H-1-Benzopyran-4-one, 2-(2-amino-3-methoxyphenyl)- & Z-100
AC1L1ISD
AC1Q6AK0
AIDS-220091
AIDS220091
AR-1C6511
BCBcMAP01_000049
Bio1_000475
Bio1_000964
Bio1_001453
Bio2_000338
Bio2_000818
BiomolKI2_000011
BiomolKI_000001
BIP0711
BMK1-B1
BRD-K62810658-001-05-6
BSPBio_000996
C093973
CCG-100605
CHEBI:150222
CHEMBL35482
EC-000.2425
EU-0101028
HMS1362B17
HMS1792B17
HMS1990B17
HMS3229M08
HMS3263M17
IDI1_002093
IN1172
KBio2_000336
KBio2_002904
KBio2_005472
KBio3_000671
KBio3_000672
KBioGR_000336
KBioSS_000336
Lopac-P-215
Lopac0_001028
LS-182409
MolPort-000-005-902
NCGC00015790-01
NCGC00015790-02
NCGC00015790-03
NCGC00015790-04
NCGC00015790-05
NCGC00015790-06
NCGC00015790-07
NCGC00015790-08
NCGC00025045-01
NCGC00025045-02
NCGC00025045-03
NCGC00025045-04
NCGC00025045-05
NCGC00179347-01
nchembio.282-comp4
NCI60_028554
NSC679828
P-215
P215_SIGMA
PD 098059
PD 98,059
PD 98059
PD 98059 & Z-100
PD 98059, PD98059
PD-098059
PD-98059
PD098059
PD09859
PD98059
PD98059-Supplied by Selleck Chemicals
S1177_Selleck
SMP2_000052
Tocris-1213
ZINC01420826

Target

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Uniprot ID:Q9UBT1_HUMAN
Synonyms:
Estrogen receptor
EC-Numbers:-
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

11713241
Evidence for estrogenic contamination of the MAPK inhibitor PD98059.. X Long; E A Gize; K Nephew; R M Bigsby (2001) Endocrinology display abstract
PD98059 blocks phosphorylation and activation of MAPK proteins, ERK1 and ERK2. In the course of examining the effect of PD98059 on estrogen-induced transcription of reporter genes in a human breast cancer cell line and in yeast, we found that two of four different batches of PD98059 produced estrogenic effects in a dose-dependent manner. In a competitive binding assay, these preparations of PD98059 displaced radiolabeled estradiol from ER alpha. Furthermore, in the yeast assay, addition of a coactivator protein, AIB1, enhanced the transcriptional effect of PD98059, indicating that it induces receptor-coactivator interactions. Although concentrations of PD98059 required to activate ER alpha in these experimental systems are 10(4)- to 10(5) higher than the concentration of estradiol required to do the same, the concentrations required to block MAPK activation are well above those which would produce maximal estrogenic effects. Thus, when PD98059 is used in estrogen-responsive cells, contaminating estrogenic activity may confound interpretation of experimental results.