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Drug-Target Interaction

Drug

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PubChem ID:2733
Structure:
Synonyms:
2(3H)-Benzoxazolone, 5-chloro-
2-Benzoxazolinone, 5-chloro-
2-Hydroxy-5-chlorobenzoxazole
32850-84-3
5-Chlorbenzoxazolin-2-on
5-chloro-1,3-benzoxazol-2(3H)-one
5-chloro-1,3-benzoxazol-2-ol
5-Chloro-2(3H)-benzoxazolone
5-Chloro-2-benzoxazolinone
5-Chloro-2-benzoxazolol
5-Chloro-2-benzoxazolone
5-Chloro-2-hydroxybenzoxazole
5-Chloro-3(H)-2-benzoxazolone
5-chloro-3H-1,3-benzoxazol-2-one
5-Chlorobenzoksazolinon-2
5-Chlorobenzoksazolinon-2 [Polish]
5-Chlorobenzoksazolon-2
5-Chlorobenzoksazolon-2 [Polish]
5-Chlorobenzoxazol-2-one
5-Chlorobenzoxazolidone
5-chlorobenzoxazolin-2-one
5-Chlorobenzoxazolone
6-Chloro-2-benzoxazolinone
95-25-0
AB00051947
AB1004047
AC-12192
AC1L1ECE
AC1Q3KM0
AC1Q3KM1
AI3-63119
AKOS000404381
BBL003952
Biomioran
BPBio1_000029
BRD-K98174813-001-05-7
BSPBio_000025
BSPBio_002019
C 4397
C07931
C2237
C4397_SIGMA
C7H4ClNO2
CAS-95-25-0
CCG-40323
CHEBI:3655
CHEBI:415123
CHEMBL1371
Chloroxazone
Chlorsoxazone
Chlorzoxane
Chlorzoxazon
chlorzoxazona
Chlorzoxazone
Chlorzoxazone (JAN/USP/INN)
Chlorzoxazone [BAN:INN:JAN]
Chlorzoxazone [INN:BAN:JAN]
Chlorzoxazonum
Chlorzoxazonum [INN-Latin]
Clorzoxazona
Clorzoxazona [INN-Spanish]
CLW
component of Parafon Forte
CPD000058269
D002753
D00771
DB00356
DivK1c_000895
EINECS 202-403-9
Escoflex
EU-0100253
EZE-DS
HMS1568B07
HMS1920O07
HMS2091E14
HMS2095B07
HMS2235I19
HMS3259I15
HMS3260D08
HMS502M17
I14-4579
IDI1_000895
KBio1_000895
KBio2_000628
KBio2_003196
KBio2_005764
KBio3_001239
KBioGR_000814
KBioSS_000628
Klorzoxazon
Lopac-C-4397
Lopac0_000253
LS-42267
McNeil Brand of Chlorzoxazone
Mioran
Miotran
MLS000069380
Myoflexin
Myoflexine
NCGC00015238-01
NCGC00015238-02
NCGC00015238-03
NCGC00015238-04
NCGC00015238-05
NCGC00015238-06
NCGC00015238-07
NCGC00015238-08
NCGC00015238-09
NCGC00015238-10
NCGC00093714-01
NCGC00093714-02
NCGC00093714-03
NCGC00093714-04
Neoflex
NINDS_000895
NSC 26189
NSC26189
Nyoflex
Ortho Brand of Chlorzoxazone
Paraflex
Paraflex (TN)
Parafon
Parafon Forte
Parafon Forte DSC
Pathorysin
Prestwick0_000163
Prestwick1_000163
Prestwick2_000163
Prestwick3_000163
Prestwick_62
Relaxazone
Remofleks
Remular
Remular-S
SAM002554888
SBB003864
SMR000058269
Solaxin
SPBio_001077
SPBio_001946
SPECTRUM1500188
Spectrum2_001149
Spectrum3_000350
Spectrum4_000287
Spectrum5_000745
Spectrum_000148
STK071582
STRIFON FORTE DSC
UNII-H0DE420U8G
Usaf ma-10
WLN: T56 BMVOJ HG
ATC-Codes:
Side-Effects:
Side-EffectFrequency
ecchymosis0
anaphylaxis0
angioedema0
petechiae0
dizziness0
gastrointestinal hemorrhage0
somnolence0
lightheadedness0
malaise0

Target

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Uniprot ID:CP1A2_HUMAN
Synonyms:
CYPIA2
Cytochrome P450 1A2
P(3)450
P450 4
P450-P3
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:2HI4
Structure:
2HI4

Binding Affinities:

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

References:

007663531
010473105
9825829
Inhibitory monoclonal antibodies to human cytochrome P450 1A2: analysis of phenacetin O-deethylation in human liver.. T J Yang; Y Sai; K W Krausz; F J Gonzalez; H V Gelboin (1998) Pharmacogenetics display abstract
Human cytochrome P450 1A2 metabolizes a large number of common drugs and engages in carcinogen metabolism and activation. Baculovirus-expressed 1A2 was used to immunize mice producing hybridomas yielding monoclonal antibodies (MAbs). Three of 2050 clones assayed yielded the MAbs, MAb 26-7-5, MAb 951-5-1, MAb 1812-2-4, which were specific for 1A2 as assessed by enzyme-linked immunosorbent assay and immunoblots. The three MAbs inhibited 1A2-catalysed metabolism of phenacetin, 7-ethoxycoumarin, chlorzoxazone and phenanthrene by more than 85%. The MAbs were highly specific to 1A2 and did not inhibit 11 other human P450s. The phenancetin O-deethylation activity varied from 0.44-2.49 nmol/min/nmol P450 in eight human liver microsomes samples. MAb 26-7-5 inhibited 1A2-dependent phenacetin O-deethylation in these samples by 64-84% indicating the amount of 1A2 contribution to this reaction and in addition a role for other P450s in the O-deethylation. Independent analysis of recombinant human P450s showed that 1A1, 1A2, 2A6 and 2C19 exhibited phenacetin O-deethylation activity, with 1A1 and 1A2 being the most active followed by 2C19 and 2A6. Eight other P450s were inactive towards phenacetin O-deethylation. The role of different P450 in eight liver samples was analysed with specific individual inhibitory MAbs. Inhibitory antibodies to 1A2, 2C8/9/18/19, 2A6, 2D6, 2E1, and 1A1 were combinatorially added to the microsomes. The O-deethylation activity was inhibited by antibodies to 1A2 (64-84%), to 2C19 (4.6-20%) and to 2A6 (0-8.8%). The total activity inhibited by antibodies to P450 2E1, 2D6 and 1A1 was less than 4.5%, indicating a minor role for these P450s in phenancetin metabolism in human liver microsomes. Thus, 1A2, 2C 9 and 2A6 are the dominant P450s for phenacetin O-deethylation. These studies demonstrate the use of inhibitory MAbs to P450s for a simple and precise assessment of the quantitative role of each P450 in the metabolism of substrates, including drugs, carcinogens, mutagens, environmental chemicals and endobiotics.