To be observed and analyzed by the network of gravitational wave detectors on ground (LIGO, VIRGO, etc.) and by the future detectors in space (LISA, etc.), inspiralling compact binaries -- binary star systems composed of neutron stars and/or black holes in their late stage of evolution -- require high-accuracy templates predicted by general relativity theory. The gravitational waves emitted by these very relativistic systems can be accurately modelled using a high-order post-Newtonian gravitational wave generation formalism. In this article, we present the current state of the art on post-Newtonian methods as applied to the dynamics and gravitational radiation of general matter sources (including the radiation reaction back onto the source) and inspiralling compact binaries. We describe the post-Newtonian equations of motion of compact binaries and the associated Lagrangian and Hamiltonian formalisms, paying attention to the self-field regularizations at work in the calculations. Several notions of innermost circular orbits are discussed. We estimate the accuracy of the post-Newtonian approximation and make a comparison with numerical computations of the gravitational self-force for compact binaries in the small mass ratio limit. The gravitational waveform and energy flux are obtained to high post-Newtonian order and the binary's orbital phase evolution is deduced from an energy balance argument. Some landmark results are given in the case of eccentric compact binaries -- moving on quasi-elliptical orbits with non-negligible eccentricity. The spins of the two black holes play an important role in the definition of the gravitational wave templates. We investigate their imprint on the equations of motion and gravitational wave phasing up to high post-Newtonian order (restricting to spin-orbit effects which are linear in spins), and analyze the post-Newtonian spin precession equations as well as the induced precession of the orbital plane.